U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C21H21F3IN3O2
Molecular Weight 531.3108
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of COBIMETINIB

SMILES

C1CCN[C@@]([H])(C1)C2(CN(C2)C(=O)c3ccc(c(c3Nc4ccc(cc4F)I)F)F)O

InChI

InChIKey=BSMCAPRUBJMWDF-KRWDZBQOSA-N
InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1

HIDE SMILES / InChI

Molecular Formula C21H21F3IN3O2
Molecular Weight 531.3108
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB05239 http://www.exelixis.com/pipeline/GDC_0973_xl518

Cobimetinib is an orally active, potent and highly selective small molecule inhibiting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), and central components of the RAS/RAF/MEK/ERK signal transduction pathway. It has been approved in Switzerland and the US, in combination with vemurafenib for the treatment of patients with unresectable or metastatic BRAF V600 mutation-positive melanoma. Preclinical studies have demonstrated that Cobimetinib is effective in inhibiting the growth of tumor cells bearing a BRAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signalling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases. Cobimetinib is used in combination with vemurafenib because the clinical benefit of a BRAF inhibitor is limited by intrinsic and acquired resistance. Reactivation of the MAPK pathway is a major contributor to treatment failure in BRAF-mutant melanomas, approximately ~80% of melanoma tumors becomes BRAF-inhibitor resistant due to reactivation of MAPK signalling. BRAF-inhibitor resistant tumor cells are sensitive to MEK inhibition, therefore cobimetinib and vemurafenib will result in dual inhibition of BRAF and its downstream target, MEK. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Cobimetinib and vemurafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Cobimetinib is used for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation. Cobimetinib is used in combination with vemurafenib, a BRAF inhibitor. Cobimetinib is marketed under the trade name Cotellic.

CNS Activity

Curator's Comment:: A tissue distribution study conducted in rats demonstrated low levels of cobimetinib in CNS tissues protected by the blood:brain barrier. COTELLIC is not recommended for patients with BRAF V600 mutation-positive melanoma who have active untreated brain metastases

Originator

Curator's Comment:: # Exelixis

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
COTELLIC

Approved Use

COTELLIC is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib.

Launch Date

1.44702715E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
273 ng/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
COBIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4340 ng × h/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
COBIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
268 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
498 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
539 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
44 h
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
COBIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
143 h
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
95.2 h
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
104 h
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
COBIMETINIB plasma
Homo sapiens
population: unhealthy
age: Adults
sex:
food status: Fasted
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
COBIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 185
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 185
Sources:
Other AEs: Lymphopenia, Lymphopenia...
Other AEs:
Lymphopenia (grade 1-2, 63%)
Lymphopenia (grade 3-4, 10%)
Sources:
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 213
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 213
Sources:
Other AEs: Creatine phosphokinase increased, Creatine phosphokinase increased...
Other AEs:
Creatine phosphokinase increased (grade 1-2, 65%)
Creatine phosphokinase increased (grade 3-4, 14%)
Sources:
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Disc. AE: Aspartate aminotransferase increased, Gamma-glutamyltransferase increased...
Other AEs: Rash, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Aspartate aminotransferase increased (2.4%)
Gamma-glutamyltransferase increased (1.6%)
Alanine aminotransferase increased (1.6%)
Rash (1.6%)
Pyrexia (1.2%)
Retinal detachment (2%)
Other AEs:
Rash (11%)
Diarrhea (9%)
Chorioretinopathy (7%)
Pyrexia (6%)
Vomiting (6%)
Nausea (5%)
Creatine phosphokinase increased (4.9%)
Diarrhea (grade 1-2, 54%)
Diarrhea (grade 3-4, 6%)
Nausea (grade 1-2, 40%)
Nausea (grade 3-4, 1%)
Vomiting (grade 1-2, 23%)
Vomiting (grade 3-4, 1%)
Stomatitis (grade 1-2, 13%)
Aphthous stomatitis (grade 1-2, 13%)
Mouth ulceration (grade 1-2, 13%)
Mucosal inflammation (grade 1-2, 13%)
Stomatitis (grade 3-4, 1%)
Aphthous stomatitis (grade 3-4, 1%)
Mouth ulceration (grade 3-4, 1%)
Mucosal inflammation (grade 3-4, 1%)
Solar dermatitis (grade 1-2, 42%)
Sunburn (grade 1-2, 42%)
Photosensitivity reaction (grade 1-2, 42%)
Solar dermatitis (grade 3-4, 4%)
Sunburn (grade 3-4, 4%)
Photosensitivity reaction (grade 3-4, 4%)
Acneiform dermatitis (grade 1-2, 14%)
Acneiform dermatitis (grade 3-4, 2%)
Pyrexia (grade 1-2, 26%)
Pyrexia (grade 3-4, 2%)
Chills (grade 1-2, 10%)
Hypertension (grade 1-2, 11%)
Hypertension (grade 3-4, 4%)
Hemorrhage (grade 1-2, 12%)
Rectal hemorrhage (grade 1-2, 12%)
Melena (grade 1-2, 12%)
Hemorrhoidal hemorrhage (grade 1-2, 12%)
Gastrointestinal hemorrhage (grade 1-2, 12%)
Hematemesis (grade 1-2, 12%)
Hematochezia (grade 1-2, 12%)
Gingival bleeding (grade 1-2, 12%)
Metrorrhagia (grade 1-2, 12%)
Uterine hemorrhage (grade 1-2, 12%)
Hemorrhagic ovarian cyst (grade 1-2, 12%)
Menometrorrhagia (grade 1-2, 12%)
Menorrhagia (grade 1-2, 12%)
Vaginal hemorrhage (grade 1-2, 12%)
Hemoptysis (grade 1-2, 12%)
Cerebral hemorrhage (grade 1-2, 12%)
Subarachnoid hemorrhage (grade 1-2, 12%)
Subgaleal hematoma (grade 1-2, 12%)
Hematuria (grade 1-2, 12%)
Epistaxis (grade 1-2, 12%)
Contusion (grade 1-2, 12%)
Traumatic hematoma (grade 1-2, 12%)
Ecchymosis (grade 1-2, 12%)
Purpura (grade 1-2, 12%)
Nail bed bleeding (grade 1-2, 12%)
Ocular hemorrhage (grade 1-2, 12%)
Eye hemorrhage (grade 1-2, 12%)
Conjunctival hemorrhage (grade 1-2, 12%)
Retinal hemorrhage (grade 1-2, 12%)
Hemorrhage (grade 3-4, 1%)
Rectal hemorrhage (grade 3-4, 1%)
Melena (grade 3-4, 1%)
Hemorrhoidal hemorrhage (grade 3-4, 1%)
Gastrointestinal hemorrhage (grade 3-4, 1%)
Hematemesis (grade 3-4, 1%)
Hematochezia (grade 3-4, 1%)
Gingival bleeding (grade 3-4, 1%)
Metrorrhagia (grade 3-4, 1%)
Uterine hemorrhage (grade 3-4, 1%)
Hemorrhagic ovarian cyst (grade 3-4, 1%)
Menometrorrhagia (grade 3-4, 1%)
Menorrhagia (grade 3-4, 1%)
Vaginal hemorrhage (grade 3-4, 1%)
Hemoptysis (grade 3-4, 1%)
Cerebral hemorrhage (grade 3-4, 1%)
Subarachnoid hemorrhage (grade 3-4, 1%)
Subgaleal hematoma (grade 3-4, 1%)
Hematuria (grade 3-4, 1%)
Epistaxis (grade 3-4, 1%)
Contusion (grade 3-4, 1%)
Traumatic hematoma (grade 3-4, 1%)
Ecchymosis (grade 3-4, 1%)
Purpura (grade 3-4, 1%)
Nail bed bleeding (grade 3-4, 1%)
Ocular hemorrhage (grade 3-4, 1%)
Eye hemorrhage (grade 3-4, 1%)
Conjunctival hemorrhage (grade 3-4, 1%)
Retinal hemorrhage (grade 3-4, 1%)
Vision blurred (grade 1-2, 14%)
Visual acuity reduced (grade 1-2, 14%)
Visual impairment (grade 1-2, 14%)
Vision blurred (grade 3-4, <1%)
Visual acuity reduced (grade 3-4, <1%)
Visual impairment (grade 3-4, <1%)
Chorioretinopathy (grade 1-2, 13%)
Chorioretinopathy (grade 3-4, <1%)
Retinal detachment (grade 1-2, 10%)
Detachment of retinal pigment epithelium (grade 1-2, 10%)
Detachment of macular retinal pigment epithelium (grade 1-2, 10%)
Retinal detachment (grade 3-4, 2%)
Detachment of retinal pigment epithelium (grade 3-4, 2%)
Detachment of macular retinal pigment epithelium (grade 3-4, 2%)
Alopecia (15%)
Hyperkeratosis (11%)
Erythema (10%)
Creatinine increased (grade 1-2, 96.3%)
Creatinine increased (grade 3-4, 3.3%)
AST increased (grade 1-2, 65%)
AST increased (grade 3-4, 8%)
ALT increased (grade 1-2, 57%)
ALT increased (grade 3-4, 11%)
Alkaline phosphatase increased (grade 1-2, 64%)
Alkaline phosphatase increased (grade 3-4, 7%)
Hypophosphatemia (grade 1-2, 56%)
Hypophosphatemia (grade 3-4, 12%)
GGT increased (grade 1-2, 44%)
GGT increased (grade 3-4, 21%)
Hyponatremia (grade 1-2, 32%)
Hyponatremia (grade 3-4, 6%)
Hypoalbuminemia (grade 1-2, 41.2%)
Hypoalbuminemia (grade 3-4, 0.8%)
Hypokalemia (grade 1-2, 20.5%)
Hypokalemia (grade 3-4, 4.5%)
Hyperkalemia (grade 1-2, 23.1%)
Hyperkalemia (grade 3-4, 2.9%)
Hypocalcemia (grade 1-2, 23.6%)
Hypocalcemia (grade 3-4, 0.4%)
Anemia (grade 1-2, 66.5%)
Anemia (grade 3-4, 2.5%)
Thrombocytopenia (grade 1-2, 18%)
Sources:
125 mg 1 times / day steady, oral
Highest studied dose
Dose: 125 mg, 1 times / day
Route: oral
Route: steady
Dose: 125 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Sources:
DLT: Rash, Central serous retinopathy...
Dose limiting toxicities:
Rash (grade 3)
Central serous retinopathy (grade 3, 2 patients)
Sources:
80 mg 1 times / day steady, oral
Highest studied dose
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
DLT: Diarrhea, Rash...
Dose limiting toxicities:
Diarrhea (grade 3, 1 patient)
Rash (grade 3, 1 patient)
Sources:
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Other AEs: Diarrhea, Diarrhea...
Other AEs:
Diarrhea (all grades, 79%)
Diarrhea (grade 3-5, 14%)
Rash (all grades, 66%)
Dermatitis acneiform (all grades, 66%)
Rash pruritic (all grades, 66%)
Generalized rash (all grades, 66%)
Dermatitis (all grades, 66%)
Exfoliative rash (all grades, 66%)
Rash erythematous (all grades, 66%)
Rash maculo-papular (all grades, 66%)
Rash (grade 3-5, 10%)
Dermatitis acneiform (grade 3-5, 10%)
Rash pruritic (grade 3-5, 10%)
Generalized rash (grade 3-5, 10%)
Dermatitis (grade 3-5, 10%)
Exfoliative rash (grade 3-5, 10%)
Rash erythematous (grade 3-5, 10%)
Rash maculo-papular (grade 3-5, 10%)
Fatigue (all grades, 66%)
Fatigue (grade 3-5, 7%)
Peripheral edema (all grades, 34%)
Periorbital edema (all grades, 34%)
Edema (all grades, 34%)
Edema face (all grades, 34%)
Nausea (all grades, 41%)
Vomiting (all grades, 48%)
Abnormal sensation in eye (all grades, 24%)
Retinal edema (all grades, 24%)
Photopsia (all grades, 24%)
Blurred vision (all grades, 24%)
Central serous retinopathy (all grades, 24%)
Vitreous floaters (all grades, 24%)
Eye disorder NOS (all grades, 24%)
Abnormal sensation in eye (grade 3-5, 3%)
Retinal edema (grade 3-5, 3%)
Photopsia (grade 3-5, 3%)
Blurred vision (grade 3-5, 3%)
Central serous retinopathy (grade 3-5, 3%)
Vitreous floaters (grade 3-5, 3%)
Eye disorder NOS (grade 3-5, 3%)
Abdominal pain upper (all grades, 35%)
Abdominal pain lower (all grades, 35%)
Abdominal discomfort (all grades, 35%)
Abdominal tenderness (all grades, 35%)
Abdominal pain upper (grade 3-5, 3%)
Abdominal pain lower (grade 3-5, 3%)
Abdominal discomfort (grade 3-5, 3%)
Abdominal tenderness (grade 3-5, 3%)
Stomatitis (all grades, 10%)
Dry skin (all grades, 10%)
Sources:
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
DLT: Rash, Dermatitis acneiform...
Other AEs: Diarrhea, Rash...
Dose limiting toxicities:
Rash (grade 3-5, 4%)
Dermatitis acneiform (grade 3-5, 4%)
Rash pruritic (grade 3-5, 4%)
Generalized rash (grade 3-5, 4%)
Dermatitis (grade 3-5, 4%)
Exfoliative rash (grade 3-5, 4%)
Rash erythematous (grade 3-5, 4%)
Rash maculo-papular (grade 3-5, 4%)
Other AEs:
Diarrhea (all grades, 56%)
Rash (all grades, 67%)
Dermatitis acneiform (all grades, 67%)
Rash pruritic (all grades, 67%)
Generalized rash (all grades, 67%)
Dermatitis (all grades, 67%)
Exfoliative rash (all grades, 67%)
Rash erythematous (all grades, 67%)
Rash maculo-papular (all grades, 67%)
Fatigue (all grades, 33%)
Fatigue (grade 3-5, 11%)
Peripheral edema (all grades, 33%)
Periorbital edema (all grades, 33%)
Edema (all grades, 33%)
Edema face (all grades, 33%)
Nausea (all grades, 22%)
Vomiting (all grades, 11%)
Abnormal sensation in eye (all grades, 15%)
Retinal edema (all grades, 15%)
Photopsia (all grades, 15%)
Blurred vision (all grades, 15%)
Central serous retinopathy (all grades, 15%)
Vitreous floaters (all grades, 15%)
Eye disorder NOS (all grades, 15%)
Stomatitis (all grades, 11%)
Dry skin (all grades, 7%)
Sources:
40 mg 1 times / day steady, oral
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
DLT: Encephalopathy...
Dose limiting toxicities:
Encephalopathy (grade 4, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Lymphopenia grade 1-2, 63%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 185
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 185
Sources:
Lymphopenia grade 3-4, 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 185
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 185
Sources:
Creatine phosphokinase increased grade 1-2, 65%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 213
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 213
Sources:
Creatine phosphokinase increased grade 3-4, 14%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 213
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 213
Sources:
Pyrexia 1.2%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Alanine aminotransferase increased 1.6%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Gamma-glutamyltransferase increased 1.6%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Rash 1.6%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Erythema 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hyperkeratosis 11%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Rash 11%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Alopecia 15%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Retinal detachment 2%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Aspartate aminotransferase increased 2.4%
Disc. AE
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Creatine phosphokinase increased 4.9%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Nausea 5%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Pyrexia 6%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vomiting 6%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Chorioretinopathy 7%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Diarrhea 9%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Chills grade 1-2, 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Detachment of macular retinal pigment epithelium grade 1-2, 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Detachment of retinal pigment epithelium grade 1-2, 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Retinal detachment grade 1-2, 10%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypertension grade 1-2, 11%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Cerebral hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Conjunctival hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Contusion grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Ecchymosis grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Epistaxis grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Eye hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Gastrointestinal hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Gingival bleeding grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematemesis grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematochezia grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematuria grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemoptysis grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhagic ovarian cyst grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhoidal hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Melena grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Menometrorrhagia grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Menorrhagia grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Metrorrhagia grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Nail bed bleeding grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Ocular hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Purpura grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Rectal hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Retinal hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Subarachnoid hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Subgaleal hematoma grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Traumatic hematoma grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Uterine hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vaginal hemorrhage grade 1-2, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Aphthous stomatitis grade 1-2, 13%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Chorioretinopathy grade 1-2, 13%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Mouth ulceration grade 1-2, 13%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Mucosal inflammation grade 1-2, 13%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Stomatitis grade 1-2, 13%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Acneiform dermatitis grade 1-2, 14%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vision blurred grade 1-2, 14%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Visual acuity reduced grade 1-2, 14%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Visual impairment grade 1-2, 14%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Thrombocytopenia grade 1-2, 18%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypokalemia grade 1-2, 20.5%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vomiting grade 1-2, 23%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hyperkalemia grade 1-2, 23.1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypocalcemia grade 1-2, 23.6%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Pyrexia grade 1-2, 26%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hyponatremia grade 1-2, 32%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Nausea grade 1-2, 40%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypoalbuminemia grade 1-2, 41.2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Photosensitivity reaction grade 1-2, 42%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Solar dermatitis grade 1-2, 42%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Sunburn grade 1-2, 42%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
GGT increased grade 1-2, 44%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Diarrhea grade 1-2, 54%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypophosphatemia grade 1-2, 56%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
ALT increased grade 1-2, 57%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Alkaline phosphatase increased grade 1-2, 64%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
AST increased grade 1-2, 65%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Anemia grade 1-2, 66.5%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Creatinine increased grade 1-2, 96.3%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypocalcemia grade 3-4, 0.4%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypoalbuminemia grade 3-4, 0.8%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Aphthous stomatitis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Cerebral hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Conjunctival hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Contusion grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Ecchymosis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Epistaxis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Eye hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Gastrointestinal hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Gingival bleeding grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematemesis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematochezia grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hematuria grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemoptysis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhagic ovarian cyst grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hemorrhoidal hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Melena grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Menometrorrhagia grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Menorrhagia grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Metrorrhagia grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Mouth ulceration grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Mucosal inflammation grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Nail bed bleeding grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Nausea grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Ocular hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Purpura grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Rectal hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Retinal hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Stomatitis grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Subarachnoid hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Subgaleal hematoma grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Traumatic hematoma grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Uterine hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vaginal hemorrhage grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vomiting grade 3-4, 1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
ALT increased grade 3-4, 11%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypophosphatemia grade 3-4, 12%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Acneiform dermatitis grade 3-4, 2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Detachment of macular retinal pigment epithelium grade 3-4, 2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Detachment of retinal pigment epithelium grade 3-4, 2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Pyrexia grade 3-4, 2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Retinal detachment grade 3-4, 2%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Anemia grade 3-4, 2.5%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hyperkalemia grade 3-4, 2.9%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
GGT increased grade 3-4, 21%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Creatinine increased grade 3-4, 3.3%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypertension grade 3-4, 4%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Photosensitivity reaction grade 3-4, 4%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Solar dermatitis grade 3-4, 4%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Sunburn grade 3-4, 4%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hypokalemia grade 3-4, 4.5%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Diarrhea grade 3-4, 6%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Hyponatremia grade 3-4, 6%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Alkaline phosphatase increased grade 3-4, 7%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
AST increased grade 3-4, 8%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Chorioretinopathy grade 3-4, <1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Vision blurred grade 3-4, <1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Visual acuity reduced grade 3-4, <1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Visual impairment grade 3-4, <1%
60 mg 1 times / day steady, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Co-administed with::
vemurafenib(960 mg twice daily on Days 1 -28)
Sources:
unhealthy, 55 years (range: 23 - 88 years)
n = 247
Health Status: unhealthy
Condition: BRAF V600 mutation-positive, unresectable or metastatic melanoma
Age Group: 55 years (range: 23 - 88 years)
Sex: M+F
Population Size: 247
Sources:
Central serous retinopathy grade 3, 2 patients
DLT, Disc. AE
125 mg 1 times / day steady, oral
Highest studied dose
Dose: 125 mg, 1 times / day
Route: oral
Route: steady
Dose: 125 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Sources:
Rash grade 3
DLT
125 mg 1 times / day steady, oral
Highest studied dose
Dose: 125 mg, 1 times / day
Route: oral
Route: steady
Dose: 125 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Sources:
Diarrhea grade 3, 1 patient
DLT
80 mg 1 times / day steady, oral
Highest studied dose
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash grade 3, 1 patient
DLT
80 mg 1 times / day steady, oral
Highest studied dose
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dry skin all grades, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Stomatitis all grades, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abnormal sensation in eye all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Blurred vision all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Central serous retinopathy all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Eye disorder NOS all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Photopsia all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Retinal edema all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Vitreous floaters all grades, 24%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Edema face all grades, 34%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Edema all grades, 34%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Periorbital edema all grades, 34%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Peripheral edema all grades, 34%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal discomfort all grades, 35%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal pain lower all grades, 35%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal pain upper all grades, 35%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal tenderness all grades, 35%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Nausea all grades, 41%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Vomiting all grades, 48%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Dermatitis acneiform all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Dermatitis all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Exfoliative rash all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Fatigue all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Generalized rash all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash erythematous all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash maculo-papular all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash pruritic all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash all grades, 66%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Diarrhea all grades, 79%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Dermatitis acneiform grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Dermatitis grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Exfoliative rash grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Generalized rash grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash erythematous grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash maculo-papular grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash pruritic grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Rash grade 3-5, 10%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Diarrhea grade 3-5, 14%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal discomfort grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal pain lower grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal pain upper grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abdominal tenderness grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Abnormal sensation in eye grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Blurred vision grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Central serous retinopathy grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Eye disorder NOS grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Photopsia grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Retinal edema grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Vitreous floaters grade 3-5, 3%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Fatigue grade 3-5, 7%
100 mg 1 times / day steady, oral
MTD
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 29
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 29
Sources:
Stomatitis all grades, 11%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Vomiting all grades, 11%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Abnormal sensation in eye all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Blurred vision all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Central serous retinopathy all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Eye disorder NOS all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Photopsia all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Retinal edema all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Vitreous floaters all grades, 15%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Nausea all grades, 22%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Edema face all grades, 33%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Edema all grades, 33%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Fatigue all grades, 33%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Periorbital edema all grades, 33%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Peripheral edema all grades, 33%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Diarrhea all grades, 56%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dermatitis acneiform all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dermatitis all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Exfoliative rash all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Generalized rash all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash erythematous all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash maculo-papular all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash pruritic all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash all grades, 67%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dry skin all grades, 7%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Fatigue grade 3-5, 11%
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dermatitis acneiform grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Dermatitis grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Exfoliative rash grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Generalized rash grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash erythematous grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash maculo-papular grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash pruritic grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Rash grade 3-5, 4%
DLT, Disc. AE
60 mg 1 times / day steady, oral
MTD
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
Encephalopathy grade 4, 1 patient
DLT, Disc. AE
40 mg 1 times / day steady, oral
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 60 years (range: 30−82 years)
n = 27
Health Status: unhealthy
Condition: metastatic or unresectable solid tumors
Age Group: 60 years (range: 30−82 years)
Sex: M+F
Population Size: 27
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 118 uM]
no [IC50 40 uM]
no [IC50 85 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no
no
no
no
yes [IC50 1.8 uM]
no (co-administration study)
Comment: Coadministration of cobimetinib 60 mg QD for 15 days with a single dose of dextromethorphan 2 mg did not change dextromethorphan exposure
Page: 38.0
yes [IC50 17 uM]
no (co-administration study)
Comment: Coadministration of cobimetinib 60 mg QD for 15 days with a single dose of midazolam 2 mg did not change midazolam exposure
Page: 38.0
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Coadministration of itraconazole 200 mg QD for 14 days with a single dose of 10 mg cobimetinib increased cobimetinib AUC by 6.7-fold (90% CI: 5.6, 8.0) and Cmax by 3.2-fold (90% CI: 2.7, 3.7) as compared with cobimetinib alone
Page: 37.0
minor
minor
minor
minor
minor
minor
minor
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Mutations of the BRAF gene in human cancer.
2002 Jun 27
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF.
2004 Mar 19
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.
2012 Jan 1
The role of BRAF V600 mutation in melanoma.
2012 Jul 9
MEK and the inhibitors: from bench to bedside.
2013 Apr 12
Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors.
2015 Nov
Cobimetinib: First Global Approval.
2015 Oct
Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cells.
2015 Sep 18
MEK inhibitors and their potential in the treatment of advanced melanoma: the advantages of combination therapy.
2016
Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans.
2016 Jan
Patents

Sample Use Guides

The recommended dose is 60 mg orally once daily for the first 21 days of each 28-day cycle until disease progression or unacceptable toxicity.
Route of Administration: Oral
Cobimetinib was shown to potently inhibit the phosphorylation of ERK and MCL-1, and to attenuate MCL-1 expression in a dose-dependent manner (2.5-10 uM) in RKO cells
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:30:21 UTC 2021
Edited
by admin
on Fri Jun 25 21:30:21 UTC 2021
Record UNII
ER29L26N1X
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
COBIMETINIB
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
COBIMETINIB [USAN]
Common Name English
XL 518
Common Name English
GDC-0973
Code English
XL-518
Common Name English
((3,4-DIFLUORO-2-(2-FLUORO-4-IODOANILINO)PHENYL)(3-HYDROXY-3-((2S)-PIPERIDIN-2-YL)AZETIDIN-1-YL)METHANONE
Common Name English
COBIMETINIB [INN]
Common Name English
XL518
Common Name English
GDC 0973
Common Name English
RG-7420
Code English
COBIMETINIB [WHO-DD]
Common Name English
COBIMETINIB [MI]
Common Name English
RG 7420
Code English
RG7420
Code English
METHANONE, (3,4-DIFLUORO-2-((2-FLUORO-4-IODOPHENYL)AMINO)PHENYL)(3-HYDROXY-3-((2S)-2-PIPERIDINYL)-1-AZETIDINYL)-
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 752820
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
WHO-ATC L01XE38
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
FDA ORPHAN DRUG 419513
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
NCI_THESAURUS C69145
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL2146883
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
NDF-RT
N0000175082
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY Kinase Inhibitors [MoA]
NCI_THESAURUS
C68923
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
RXCUI
1722365
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY RxNorm
PUBCHEM
16222096
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
EVMPD
SUB122319
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
INN
9645
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
FDA UNII
ER29L26N1X
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
MERCK INDEX
M11872
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
LACTMED
Cobimetinib
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
DRUG CENTRAL
5046
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
ChEMBL
CHEMBL3330650
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
DRUG BANK
DB05239
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
CAS
934660-93-2
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
WIKIPEDIA
Cobimetinib
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
EPA CompTox
934660-93-2
Created by admin on Fri Jun 25 21:30:22 UTC 2021 , Edited by admin on Fri Jun 25 21:30:22 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
Amount recovered in the feces of healthy subjects after a single dose of 20 mg Cobimetinib
FECAL
TARGET -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
Cobimetinib is a reversible inhibitor of CYP3A4 and CYP2D6 in vitro.
REVERSIBLE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> INHIBITOR
Cobimetinib is a reversible inhibitor of CYP3A4 and CYP2D6 in vitro.
REVERSIBLE
EXCRETED UNCHANGED
Amount recovered in the urine of healthy subjects after a single dose of 20 mg Cobimetinib
URINE
METABOLIC ENZYME -> INHIBITOR
Cobimetinib is a time-dependent inhibitor of CYP3A4 in vitro.
TIME-DEPENDENT INHIBITION
METABOLIC ENZYME -> SUBSTRATE
CONJUGATE -> PARENT
Related Record Type Details
METABOLITE -> PARENT
METABOLITE INACTIVE -> PARENT
METABOLITE -> PARENT
Four hours after a Single Dose of 20 mg Cobimetinib in Healthy Subjects
PLASMA
METABOLITE -> PARENT
Glycine conjugate of the hydrolyzed product after a single dose of 20 mg Cobimetinib
URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

ONCE DAILY DOSE

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC