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Details

Stereochemistry ACHIRAL
Molecular Formula C17H15BrF2N4O3
Molecular Weight 441.227
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BINIMETINIB

SMILES

Cn1cnc2c1cc(c(c2F)Nc3ccc(cc3F)Br)C(=NOCCO)O

InChI

InChIKey=ACWZRVQXLIRSDF-UHFFFAOYSA-N
InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

HIDE SMILES / InChI

Description
Curator's Comment:: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C84865 | https://www.ncbi.nlm.nih.gov/pubmed/23635776 | https://acr.confex.com/acr/2006/webprogram/Paper5558.html

Binimetinib (MEK162) is an oral small-molecule with potential antineoplastic activity. It is a selective mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, a key protein kinase in the RAS/RAF/MEK/ERK pathway, which regulates several key cellular activities including proliferation, differentiation, migration, survival and angiogenesis. Inappropriate activation of this pathway has been shown to occur in many cancers, in particular through mutations in BRAF, KRAS and NRAS. MEK162 at 6 mg/kg, BID combined with BEZ235 (dual PI3K/mTOR inhibitor) resulted in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. There are three ongoing Phase 3 trials with binimetinib in advanced cancer patients: NEMO (NRAS-mutant melanoma), COLUMBUS (encorafenib in combination with binimetinib in BRAF-mutant melanoma) and BEACON CRC (encorafenib, binimetinib and cetuximab in BRAF-mutant colorectal cancer).

CNS Activity

Curator's Comment:: Preclinical studies of MEK162 in patients with the BRAF fusion gene have revealed that this novel drug might be able to penetrate the blood-brain barrier, which has encouraged investigators to explore this therapeutic candidate.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
MEKTOVI

Approved Use

is indicated, in combination with encorafenib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test

Launch Date

1.52997121E12
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
545 ng/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BINIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
241 ng/mL
45 mg 2 times / day multiple, oral
dose: 45 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BINIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1710 ng × h/mL
60 mg 2 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BINIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
964 ng × h/mL
45 mg 2 times / day multiple, oral
dose: 45 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BINIMETINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
DLT: Chorioretinopathy, Dermatitis acneiform...
Disc. AE: Macular oedema, Nausea...
Other AEs: Retinal deposits, Retinopathy...
Dose limiting toxicities:
Chorioretinopathy (grade 3, 25%)
Dermatitis acneiform (grade 3, 25%)
AEs leading to
discontinuation/dose reduction:
Macular oedema (grade 3-4, 25%)
Nausea (grade 1-2, 25%)
Vomiting (grade 1-2, 50%)
Fatigue (grade 1-2, 25%)
Other AEs:
Retinal deposits (grade 3-4, 25%)
Retinopathy (grade 3-4, 25%)
Papilloedema (grade 3-4, 25%)
Retinal detachment (grade 3-4, 25%)
Retinal disorder (grade 3-4, 25%)
Acne (grade 3-4, 25%)
Skin exfoliation (grade 3-4, 25%)
Diarrhoea (grade 1-2, 25%)
Peripheral oedema (grade 1-2, 50%)
Abdominal pain (grade 1-2, 25%)
Anorexia (grade 1-2, 25%)
Dyspnoea (grade 1-2, 25%)
Sources:
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Disc. AE: Dermatitis acneiform, Acne...
Other AEs: Diarrhoea, Peripheral oedema...
AEs leading to
discontinuation/dose reduction:
Dermatitis acneiform (grade 1-2, 85%)
Acne (grade 1-2, 85%)
Skin exfoliation (grade 1-2, 85%)
Dermatitis acneiform (grade 3-4, 2%)
Acne (grade 3-4, 2%)
Skin exfoliation (grade 3-4, 2%)
Nausea (grade 1-2, 51%)
Vomiting (grade 1-2, 49%)
Fatigue (grade 1-2, 39%)
Fatigue (grade 3-4, 2%)
Other AEs:
Diarrhoea (grade 1-2, 61%)
Peripheral oedema (grade 1-2, 51%)
Anaemia (grade 1-2, 12%)
Anaemia (grade 3-4, 24%)
Abdominal pain (grade 1-2, 17%)
Abdominal pain (grade 3-4, 7%)
Anorexia (grade 1-2, 20%)
Constipation (grade 1-2, 20%)
Constipation (grade 3-4, 5%)
Dyspnoea (grade 1-2, 15%)
Dyspnoea (grade 3-4, 2%)
Pyrexia (grade 1-2, 17%)
Pyrexia (grade 3-4, 2%)
Dizziness (grade 1-2, 22%)
Pulmonary embolism (grade 4, 1 patient)
Generalised oedema (grade 4, 1 patient)
Sources:
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Disc. AE: Retinal deposits, Retinopathy...
Other AEs: Papilloedema, Retinal disorder...
AEs leading to
discontinuation/dose reduction:
Retinal deposits (grade 1-2, 27%)
Retinopathy (grade 1-2, 27%)
Chorioretinopathy (grade 1-2, 27%)
Macular oedema (grade 1-2, 27%)
Retinal detachment (grade 1-2, 27%)
Other AEs:
Papilloedema (grade 1-2, 27%)
Retinal disorder (grade 1-2, 27%)
Sources:
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Disc. AE: Chorioretinopathy, Macular oedema...
Other AEs: Retinal deposits, Retinopathy...
AEs leading to
discontinuation/dose reduction:
Chorioretinopathy (grade 1-2, 11%)
Macular oedema (grade 1-2, 11%)
Retinal detachment (grade 1-2, 11%)
Dermatitis acneiform (grade 1-2, 75%)
Acne (grade 1-2, 75%)
Skin exfoliation (grade 1-2, 75%)
Dermatitis acneiform (grade 3-4, 2%)
Acne (grade 3-4, 2%)
Skin exfoliation (grade 3-4, 2%)
Nausea (grade 1-2, 61%)
Vomiting (grade 1-2, 52%)
Diarrhoea (grade 1-2, 39%)
Fatigue (grade 1-2, 41%)
Fatigue (grade 3-4, 5%)
Other AEs:
Retinal deposits (grade 1-2, 11%)
Retinopathy (grade 1-2, 11%)
Papilloedema (grade 1-2, 11%)
Retinal disorder (grade 1-2, 11%)
Peripheral oedema (grade 1-2, 45%)
Anaemia (grade 1-2, 11%)
Anaemia (grade 3-4, 7%)
Abdominal pain (grade 1-2, 16%)
Abdominal pain (grade 3-4, 2%)
Anorexia (grade 1-2, 18%)
Constipation (grade 1-2, 14%)
Dyspnoea (grade 1-2, 11%)
Dyspnoea (grade 3-4, 5%)
Pyrexia (grade 1-2, 16%)
Dizziness (grade 1-2, 11%)
Sources:
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Disc. AE: Left ventricular dysfunction, Serous retinopathy...
Other AEs: Fatigue, Pyrexia...
AEs leading to
discontinuation/dose reduction:
Left ventricular dysfunction (6%)
Serous retinopathy (5%)
Left ventricular dysfunction (3%)
Serous retinopathy (3%)
Colitis (2%)
Hemorrhage (2%)
Headache (1%)
Other AEs:
Fatigue (grade 3-4, 3%)
Pyrexia (grade 3-4, 4%)
Peripheral edema (grade 3-4, 1%)
Fatigue (all grades, 43%)
Pyrexia (all grades, 18%)
Peripheral edema (all grades, 13%)
Nausea (grade 3-4, 2%)
Diarrhea (grade 3-4, 3%)
Vomiting (grade 3-4, 2%)
Abdominal pain (grade 3-4, 4%)
Nausea (all grades, 41%)
Diarrhea (all grades, 36%)
Vomiting (all grades, 30%)
Abdominal pain (all grades, 28%)
Constipation (all grades, 22%)
Rash (grade 3-4, 1%)
Rash (all grades, 22%)
Dizziness (grade 3-4, 3%)
Dizziness (all grades, 15%)
Visual impairment (all grades, 20%)
Serous retinopathy (grade 3-4, 3%)
Serous retinopathy (all grades, 20%)
Hemorrhage (grade 3-4, 3%)
Hemorrhage (all grades, 19%)
Hypertension (grade 3-4, 6%)
Hypertension (all grades, 11%)
Anemia (grade 3-4, 3.6%)
Anemia (all grades, 36%)
Leukopenia (all grades, 13%)
Lymphopenia (grade 3-4, 2.1%)
Lymphopenia (all grades, 13%)
Neutropenia (grade 3-4, 3.1%)
Neutropenia (all grades, 13%)
Creatinine increased (grade 3-4, 3.6%)
Creatinine increased (all grades, 93%)
Creatine phosphokinase increased (grade 3-4, 5%)
Creatine phosphokinase increased (all grades, 58%)
Gamma-glutamyltransferase increased (grade 3-4, 11%)
Gamma-glutamyltransferase increased (all grades, 45%)
ALT increased (grade 3-4, 6%)
ALT increased (all grades, 29%)
AST increased (grade 3-4, 2.6%)
AST increased (all grades, 27%)
Alkaline phosphatase increased (grade 3-4, 0.5%)
Alkaline phosphatase increased (all grades, 21%)
Hyponatremia (grade 3-4, 3.6%)
Hyponatremia (all grades, 18%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Abdominal pain grade 1-2, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Anorexia grade 1-2, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Diarrhoea grade 1-2, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Dyspnoea grade 1-2, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Fatigue grade 1-2, 25%
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Nausea grade 1-2, 25%
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Peripheral oedema grade 1-2, 50%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Vomiting grade 1-2, 50%
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Chorioretinopathy grade 3, 25%
DLT, Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Dermatitis acneiform grade 3, 25%
DLT, Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Acne grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Papilloedema grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Retinal deposits grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Retinal detachment grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Retinal disorder grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Retinopathy grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Skin exfoliation grade 3-4, 25%
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Macular oedema grade 3-4, 25%
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 4
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 4
Sources:
Anaemia grade 1-2, 12%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Dyspnoea grade 1-2, 15%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Abdominal pain grade 1-2, 17%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Pyrexia grade 1-2, 17%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Anorexia grade 1-2, 20%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Constipation grade 1-2, 20%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Dizziness grade 1-2, 22%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Fatigue grade 1-2, 39%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Vomiting grade 1-2, 49%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Peripheral oedema grade 1-2, 51%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Nausea grade 1-2, 51%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Diarrhoea grade 1-2, 61%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Acne grade 1-2, 85%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Dermatitis acneiform grade 1-2, 85%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Skin exfoliation grade 1-2, 85%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Dyspnoea grade 3-4, 2%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Pyrexia grade 3-4, 2%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Acne grade 3-4, 2%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Dermatitis acneiform grade 3-4, 2%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Fatigue grade 3-4, 2%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Skin exfoliation grade 3-4, 2%
Disc. AE
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Anaemia grade 3-4, 24%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Constipation grade 3-4, 5%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Abdominal pain grade 3-4, 7%
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Generalised oedema grade 4, 1 patient
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Pulmonary embolism grade 4, 1 patient
60 mg 2 times / day steady, oral
MTD
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Papilloedema grade 1-2, 27%
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Retinal disorder grade 1-2, 27%
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Chorioretinopathy grade 1-2, 27%
Disc. AE
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Macular oedema grade 1-2, 27%
Disc. AE
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Retinal deposits grade 1-2, 27%
Disc. AE
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Retinal detachment grade 1-2, 27%
Disc. AE
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Retinopathy grade 1-2, 27%
Disc. AE
60 mg 2 times / day steady, oral
MTD
unhealthy, 58 years (range: 30–86 years)
n = 41
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 41
Sources:
Anaemia grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Dizziness grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Dyspnoea grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Papilloedema grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Retinal deposits grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Retinal disorder grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Retinopathy grade 1-2, 11%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Chorioretinopathy grade 1-2, 11%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Macular oedema grade 1-2, 11%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Retinal detachment grade 1-2, 11%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Constipation grade 1-2, 14%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Abdominal pain grade 1-2, 16%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Pyrexia grade 1-2, 16%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Anorexia grade 1-2, 18%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Diarrhoea grade 1-2, 39%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Fatigue grade 1-2, 41%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Peripheral oedema grade 1-2, 45%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Vomiting grade 1-2, 52%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Nausea grade 1-2, 61%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Acne grade 1-2, 75%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Dermatitis acneiform grade 1-2, 75%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Skin exfoliation grade 1-2, 75%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Abdominal pain grade 3-4, 2%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Acne grade 3-4, 2%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Dermatitis acneiform grade 3-4, 2%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Skin exfoliation grade 3-4, 2%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Dyspnoea grade 3-4, 5%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Fatigue grade 3-4, 5%
Disc. AE
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Anaemia grade 3-4, 7%
45 mg 2 times / day steady, oral
RP2D
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Sources:
unhealthy, 58 years (range: 30–86 years)
n = 44
Health Status: unhealthy
Condition: biliary cancer| KRAS-mutant colorectal cancer
Age Group: 58 years (range: 30–86 years)
Sex: M+F
Population Size: 44
Sources:
Headache 1%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Colitis 2%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hemorrhage 2%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Left ventricular dysfunction 3%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Serous retinopathy 3%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Serous retinopathy 5%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Left ventricular dysfunction 6%
Disc. AE
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hypertension all grades, 11%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Leukopenia all grades, 13%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Lymphopenia all grades, 13%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Neutropenia all grades, 13%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Peripheral edema all grades, 13%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Dizziness all grades, 15%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hyponatremia all grades, 18%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Pyrexia all grades, 18%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hemorrhage all grades, 19%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Serous retinopathy all grades, 20%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Visual impairment all grades, 20%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Alkaline phosphatase increased all grades, 21%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Constipation all grades, 22%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Rash all grades, 22%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
AST increased all grades, 27%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Abdominal pain all grades, 28%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
ALT increased all grades, 29%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Vomiting all grades, 30%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Anemia all grades, 36%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Diarrhea all grades, 36%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Nausea all grades, 41%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Fatigue all grades, 43%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Gamma-glutamyltransferase increased all grades, 45%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Creatine phosphokinase increased all grades, 58%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Creatinine increased all grades, 93%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Alkaline phosphatase increased grade 3-4, 0.5%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Peripheral edema grade 3-4, 1%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Rash grade 3-4, 1%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Gamma-glutamyltransferase increased grade 3-4, 11%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Nausea grade 3-4, 2%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Vomiting grade 3-4, 2%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Lymphopenia grade 3-4, 2.1%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
AST increased grade 3-4, 2.6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Diarrhea grade 3-4, 3%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Dizziness grade 3-4, 3%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Fatigue grade 3-4, 3%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hemorrhage grade 3-4, 3%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Serous retinopathy grade 3-4, 3%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Neutropenia grade 3-4, 3.1%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Anemia grade 3-4, 3.6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Creatinine increased grade 3-4, 3.6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hyponatremia grade 3-4, 3.6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Abdominal pain grade 3-4, 4%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Pyrexia grade 3-4, 4%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Creatine phosphokinase increased grade 3-4, 5%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
ALT increased grade 3-4, 6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
Hypertension grade 3-4, 6%
45 mg 2 times / day steady, oral
Recommended
Dose: 45 mg, 2 times / day
Route: oral
Route: steady
Dose: 45 mg, 2 times / day
Co-administed with::
encorafenib(450 mg once daily)
Sources:
unhealthy
n = 192
Health Status: unhealthy
Condition: BRAF V600 mutation-positive unresectable or metastatic melanoma
Population Size: 192
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
weak [IC50 18.1 uM]
weak [IC50 50 uM]
weak [IC50 50 uM]
weak [IC50 >25 uM]
weak
unlikely
Comment: It is not expected for binimetinib to have a clinically relevant induction of CYP2C9, as the plasma concentrations observed in patients is well below the concentration required for minimal induction of CYP2C9 based on in vitro study
Page: -
yes [IC50 6 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
major
major
no (co-administration study)
Comment: atazanavir did not alter the exposure of BINIMETINIB
Page: -
no
no
no
no
no
no
no (co-administration study)
Comment: did not alter the exposure of midazolam
Page: -
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
MEK and the inhibitors: from bench to bedside.
2013 Apr 12
RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer.
2013 Jun
MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study.
2013 Mar
Adjuvant immunotherapy of melanoma and development of new approaches using the neoadjuvant approach.
2013 May-Jun
MEK1/2 inhibitors in the treatment of gynecologic malignancies.
2014 Apr
MEK targeting in N-RAS mutated metastatic melanoma.
2014 Mar 4
Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations.
2014 Sep 25
Patents

Patents

Sample Use Guides

MEK162 administered as a fixed dose of 45 mg (3 x 15 mg tablets) BID, with a glass of water and taken with or without food.
Route of Administration: Oral
MCF7 (mutant PIK3CA) breast cancer cells exhibiting sensitivity to PI3K inhibition were seeded in 12-well plates (2 × 10^4). After 24 hours, cells were treated with BEZ235, BKM120, GDC-0941, or MK2206 alone or in combination with MEK162. MEK162 (1 uM) combined with MK-2206 (2 mM) completely reversed the resistance of RSK-expressing MCF7 cells.
Name Type Language
BINIMETINIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
5-((4-BROMO-2-FLUOROPHENYLAMINO)-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZO (D) IMIDAZOLE-6-CARBOXAMIDE
Systematic Name English
5-((4-BROMO-2-FLUOROPHENYL)AMINO)-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZIMIDAZOLE-6-CARBOXAMIDE
Systematic Name English
BINIMETINIB [INN]
Common Name English
BINIMETINIB [USAN]
Common Name English
BINIMETINIB [JAN]
Common Name English
MEK162
Code English
ARRY-438162
Code English
MEKTOVI
Brand Name English
BINIMETINIB [MI]
Common Name English
NVP-MEK162
Code English
1H-BENZIMIDAZOLE-6-CARBOXAMIDE, 5-((4-BROMO-2-FLUOROPHENYL)AMINO)-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-
Systematic Name English
ARRY-162
Code English
BINIMETINIB [ORANGE BOOK]
Common Name English
BINIMETINIB [WHO-DD]
Common Name English
5-(4-BROMO-2-FLUOROPHENYLAMINO)-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZO(D)IMIDAZOLE-6-CARBOXAMIDE
Systematic Name English
ARRY 438162
Code English
MEK-162
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 411613
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
NCI_THESAURUS C69145
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
WHO-ATC L01XE41
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
FDA ORPHAN DRUG 411513
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
FDA ORPHAN DRUG 440414
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C84865
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
EVMPD
SUB179942
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
INN
9764
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
CAS
606143-89-9
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
DRUG CENTRAL
5290
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
MERCK INDEX
M12078
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
PUBCHEM
10288191
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
FDA UNII
181R97MR71
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
EPA CompTox
606143-89-9
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
WIKIPEDIA
Binimetinib
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
LACTMED
Binimetinib
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
ChEMBL
CHEMBL3187723
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
RXCUI
2049122
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY
DRUG BANK
DB11967
Created by admin on Sat Jun 26 16:37:30 UTC 2021 , Edited by admin on Sat Jun 26 16:37:30 UTC 2021
PRIMARY