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Details

Stereochemistry ACHIRAL
Molecular Formula C23H18ClF2N3O3S
Molecular Weight 489.922
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VEMURAFENIB

SMILES

CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(Cl)C=C4)=C(F)C=C1

InChI

InChIKey=GPXBXXGIAQBQNI-UHFFFAOYSA-N
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)

HIDE SMILES / InChI

Molecular Formula C23H18ClF2N3O3S
Molecular Weight 489.922
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://www.webmd.com/melanoma-skin-cancer/news/20110817/zelboraf-approved-for-late-stage-melanoma

Vemurafenib (trade name Zelboraf) is a low molecular weight, orally available kinase inhibitor. It inhibits of some mutated forms of BRAF serinethreonine kinase, including BRAF V600E and is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5 and FGR at similar concentrations. Vemurafenib is not recommended for use in patients with wild-type BRAF melanoma. Zelboraf does not cure melanoma, but stops it's progression. Some 26% of patients in clinical trials developed a non melanoma form of skin cancer called cutaneous squamous cell carcinoma, which can usually be removed via relatively simple surgery. Other side effects include joint pain, rash, hair loss, fatigue, nausea, and skin sensitivity to sunlight. Patients taking Zelboraf must avoid sun exposure. It's not yet clear how long Zelboraf can increase melanoma survival.

CNS Activity

Curator's Comment: There are emerging data indicating that vemurafenib can penetrate CNS but they are not conclusive: https://www.ncbi.nlm.nih.gov/pubmed/?term=23036672

Originator

Curator's Comment: Initially developed by Plexxikon Inc., a member of the Daiichi Sankyo Group of pharmaceutical companies the drug is being co-marketed by Genentech, a division of Roche.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
31.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
ZELBORAF

Approved Use

Indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. Limitation of Use: ZELBORAF is not indicated for treatment of patients with wild-type BRAF melanoma.

Launch Date

2011
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
52.7 μg/mL
720 mg 2 times / day multiple, oral
dose: 720 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
35.4 μg/mL
480 mg 2 times / day multiple, oral
dose: 480 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.8 μg/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.4 μg/mL
720 mg single, oral
dose: 720 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.6 μg/mL
480 mg single, oral
dose: 480 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.9 μg/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
62 μg/mL
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
17.2 μg/mL
240 mg 2 times / day multiple, oral
dose: 240 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
61.4 μg/mL
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3127.1 μg × h/mL
720 mg 2 times / day multiple, oral
dose: 720 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2243.5 μg × h/mL
480 mg 2 times / day multiple, oral
dose: 480 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
27 μg × h/mL
960 mg single, oral
dose: 960 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
21.9 μg × h/mL
720 mg single, oral
dose: 720 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13.8 μg × h/mL
480 mg single, oral
dose: 480 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
8.3 μg × h/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
601 μg × h/mL
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
920.3 μg × h/mL
240 mg 2 times / day multiple, oral
dose: 240 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3530.3 μg × h/mL
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
34.9 h
720 mg 2 times / day multiple, oral
dose: 720 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
38.4 h
480 mg 2 times / day multiple, oral
dose: 480 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
31.5 h
240 mg 2 times / day multiple, oral
dose: 240 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
34.1 h
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
960 mg 2 times / day multiple, oral
dose: 960 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VEMURAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Other AEs: Rash, Photosensitivity reaction...
Other AEs:
Rash (grade 3, 8%)
Photosensitivity reaction (grade 3, 3%)
Alopecia (grade 3, <1%)
Pruritus (grade 3, 1%)
Hyperkeratosis (grade 3, 1%)
Rash maculo-papular (grade 3, 2%)
Rash papular (grade 3, <1%)
Arthralgia (grade 3, 4%)
Myalgia (grade 3, <1%)
Pain in extremity (grade 3, <1%)
Back pain (grade 3, <1%)
Fatigue (grade 3, 2%)
Edema peripheral (grade 3, <1%)
Pyrexia (grade 3, <1%)
Asthenia (grade 3, <1%)
Nausea (grade 3, 2%)
Diarrhea (grade 3, <1%)
Vomiting (grade 3, 1%)
Constipation (grade 3, <1%)
Headache (grade 3, <1%)
Skin papilloma (grade 3, <1%)
Squamous cell carcinoma of skin (grade 3, 22%)
Seborrheic keratosis (grade 3, <1%)
GGT increased (grade 3, 3%)
Rash (37%)
Photosensitivity reaction (33%)
Alopecia (45%)
Pruritus (23%)
Hyperkeratosis (24%)
Rash maculo-papular (9%)
Actinic keratosis (8%)
Dry skin (19%)
Rash papular (5%)
Erythema (14%)
Arthralgia (53%)
Myalgia (13%)
Pain in extremity (18%)
Musculoskeletal pain (8%)
Back pain (8%)
Fatigue (38%)
Edema peripheral (17%)
Pyrexia (19%)
Asthenia (11%)
Nausea (35%)
Diarrhea (28%)
Vomiting (18%)
Constipation (12%)
Headache (23%)
Dysgeusia (14%)
Skin papilloma (21%)
Squamous cell carcinoma of skin (24%)
Seborrheic keratosis (10%)
GGT increased (5%)
Decreased appetite (18%)
Cough (8%)
Sunburn (10%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Disc. AE: Arthralgia, Dysphagia...
AEs leading to
discontinuation/dose reduction:
Arthralgia (2%)
Dysphagia (2%)
Pneumonia (2%)
Brain metastases (1%)
Dyspnea (1%)
Pneumonia (1%)
Thrombocytopenia (1%)
Abdominal pain (1%)
Aortic aneurysm rupture (1%)
Ascites (1%)
Atrial fibrillation (1%)
Blood alkaline phosphatase increased (1%)
Blood bilirubin increased (1%)
Chest pain (1%)
Choking (1%)
Cognitive disorder (1%)
Hyperemia of conjunctiva (1%)
Dehydration (1%)
Diplopia (1%)
Dyspepsia (1%)
Esophageal pain (1%)
Fatigue (1%)
Gait disturbance (1%)
GGT increased (1%)
Gastroesophageal reflux (1%)
Hepatitis acute (1%)
Hyponatremia (1%)
Intracranial tumor hemorrhage (1%)
Myocardial infarction (1%)
Pain (1%)
Pancreatitis (1%)
Rash (1%)
Renal impairment (1%)
Stevens-Johnson syndrome (1%)
Thrombocytopenia (1%)
Toxic skin eruption (1%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Other AEs: LDH increased, Alkaline phosphatase increased...
Other AEs:
LDH increased (grade 3, 2.7%)
Alkaline phosphatase increased (grade 3, 3%)
ALT increased (grade 3, 2.7%)
GGT increased (grade 3, 11.3%)
AST increased (grade 3, <1%)
Bilirubin increased (grade 3, 1.8%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Other AEs: Arthritis, Joint effusion...
Other AEs:
Arthritis (grade 3, <1%)
Joint effusion (grade 3, <1%)
Atrial fibrillation (grade 3, <1%)
Myocardial infarction (grade 3, <1%)
Pericarditis (grade 3, <1%)
QT interval prolonged (grade 3, 2.1%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Other AEs: Rash, Keratoacanthoma...
Other AEs:
Rash (grade 3, 8.3%)
Keratoacanthoma (grade 3, 8.6%)
Arthralgia (grade 3, 4.5%)
GGT increased (grade 3, 3.3%)
Photosensitivity reaction (grade 3, 2.7%)
Maculopapular rash (grade 3, 2.4%)
Blood alkaline phosphatase increased (grade 3, 2.7%)
Fatigue (grade 3, 2.1%)
Dyspnea (grade 3, 2.1%)
Nausea (grade 3, 2.1%)
ALT increased (grade 3, 1.8%)
Pain in extremity (grade 3, 1.5%)
Pruritus (grade 3, 1.5%)
Vomiting (grade 3, 1.2%)
Pain (grade 3, 1.2%)
Blood bilirubin increased (grade 3, 1.2%)
Hyperkeratosis (grade 3, 1.2%)
Anemia (grade 3, <1%)
Thrombocytopenia (grade 3, <1%)
Neutropenia (grade 3, <1%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Other AEs: Hyperglycemia, Creatinine increased...
Other AEs:
Hyperglycemia (grade 3, 2.1%)
Creatinine increased (grade 3, 1.5%)
Hyperkalemia (grade 3, 1.2%)
Hypercalcemia (grade 3, 2%)
Decreased hemoglobin (grade 3, 3.7%)
Lymphocyte count decreased (grade 3, 8.3%)
Hypoalbuminemia (grade 3, 1.3%)
Hypophosphatemia (grade 3, 3.5%)
Neutrophil count decreased (grade 3, <1%)
WBC decreased (grade 3, <1%)
Platelets decreased (grade 3, <1%)
Sources:
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Other AEs: Arthralgia, Rash...
Other AEs:
Arthralgia (grade 3, 3%)
Rash (grade 3, 3%)
Squamous cell carcinoma, keratoacanthoma-type (grade 3, 31%)
Nausea (grade 3, 3%)
Fatigue (grade 3, 6%)
Photosensitivity reaction (grade 3, 3%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 6%)
Sources:
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
DLT: Arthralgia, Rash...
Other AEs: Squamous cell carcinoma, keratoacanthoma-type, Fatigue...
Dose limiting toxicities:
Arthralgia (grade 3, 17%)
Rash (grade 3, 50%)
Other AEs:
Squamous cell carcinoma, keratoacanthoma-type (grade 3, 33%)
Fatigue (grade 3, 33%)
Pruritus (grade 3, 17%)
Lymphopenia (grade 3, 17%)
Sources:
240 mg 2 times / day multiple, oral
Dose: 240 mg, 2 times / day
Route: oral
Route: multiple
Dose: 240 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Other AEs: Squamous cell carcinoma, keratoacanthoma-type...
Other AEs:
Squamous cell carcinoma, keratoacanthoma-type (grade 3, 50%)
Sources:
360 mg 2 times / day multiple, oral
Dose: 360 mg, 2 times / day
Route: oral
Route: multiple
Dose: 360 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Other AEs: Squamous cell carcinoma, keratoacanthoma-type...
Other AEs:
Squamous cell carcinoma, keratoacanthoma-type (grade 3, 38%)
Sources:
1600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1600 mg, 2 times / day
Sources:
unhealthy
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy
DLT: Rash, Fatigue...
Dose limiting toxicities:
Rash (60%)
Fatigue (60%)
Sources:
360 mg 2 times / day multiple, oral
Dose: 360 mg, 2 times / day
Route: oral
Route: multiple
Dose: 360 mg, 2 times / day
Sources:
unhealthy
Other AEs: ALT increased...
Other AEs:
ALT increased (grade 3)
Sources:
720 mg 2 times / day multiple, oral
Dose: 720 mg, 2 times / day
Route: oral
Route: multiple
Dose: 720 mg, 2 times / day
Sources:
unhealthy
DLT: Pancytopenia...
Dose limiting toxicities:
Pancytopenia (grade 4)
Sources:
AEs

AEs

AESignificanceDosePopulation
Seborrheic keratosis 10%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Sunburn 10%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Asthenia 11%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Constipation 12%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Myalgia 13%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Dysgeusia 14%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Erythema 14%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Edema peripheral 17%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Decreased appetite 18%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pain in extremity 18%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Vomiting 18%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Dry skin 19%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pyrexia 19%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Skin papilloma 21%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Headache 23%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pruritus 23%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Hyperkeratosis 24%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Squamous cell carcinoma of skin 24%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Diarrhea 28%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Photosensitivity reaction 33%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Nausea 35%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash 37%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Fatigue 38%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Alopecia 45%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
GGT increased 5%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash papular 5%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Arthralgia 53%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Actinic keratosis 8%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Back pain 8%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Cough 8%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Musculoskeletal pain 8%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash maculo-papular 9%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Hyperkeratosis grade 3, 1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pruritus grade 3, 1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Vomiting grade 3, 1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Fatigue grade 3, 2%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Nausea grade 3, 2%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash maculo-papular grade 3, 2%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Squamous cell carcinoma of skin grade 3, 22%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
GGT increased grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Photosensitivity reaction grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Arthralgia grade 3, 4%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash grade 3, 8%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Alopecia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Asthenia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Back pain grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Constipation grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Diarrhea grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Edema peripheral grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Headache grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Myalgia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pain in extremity grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Pyrexia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Rash papular grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Seborrheic keratosis grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Skin papilloma grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
unhealthy, median age was 54 years
Abdominal pain 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Aortic aneurysm rupture 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Ascites 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Atrial fibrillation 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Blood alkaline phosphatase increased 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Blood bilirubin increased 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Brain metastases 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Chest pain 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Choking 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Cognitive disorder 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Dehydration 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Diplopia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Dyspepsia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Dyspnea 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Esophageal pain 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Fatigue 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
GGT increased 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Gait disturbance 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Gastroesophageal reflux 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hepatitis acute 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hyperemia of conjunctiva 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hyponatremia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Intracranial tumor hemorrhage 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Myocardial infarction 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pain 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pancreatitis 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pneumonia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Rash 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Renal impairment 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Stevens-Johnson syndrome 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Thrombocytopenia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Thrombocytopenia 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Toxic skin eruption 1%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Arthralgia 2%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Dysphagia 2%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pneumonia 2%
Disc. AE
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Bilirubin increased grade 3, 1.8%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
GGT increased grade 3, 11.3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
ALT increased grade 3, 2.7%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
LDH increased grade 3, 2.7%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Alkaline phosphatase increased grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
AST increased grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
QT interval prolonged grade 3, 2.1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Arthritis grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Atrial fibrillation grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Joint effusion grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Myocardial infarction grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pericarditis grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Blood bilirubin increased grade 3, 1.2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hyperkeratosis grade 3, 1.2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pain grade 3, 1.2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Vomiting grade 3, 1.2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pain in extremity grade 3, 1.5%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Pruritus grade 3, 1.5%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
ALT increased grade 3, 1.8%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Dyspnea grade 3, 2.1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Fatigue grade 3, 2.1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Nausea grade 3, 2.1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Maculopapular rash grade 3, 2.4%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Blood alkaline phosphatase increased grade 3, 2.7%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Photosensitivity reaction grade 3, 2.7%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
GGT increased grade 3, 3.3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Arthralgia grade 3, 4.5%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Rash grade 3, 8.3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Keratoacanthoma grade 3, 8.6%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Anemia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Neutropenia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Thrombocytopenia grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hyperkalemia grade 3, 1.2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hypoalbuminemia grade 3, 1.3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Creatinine increased grade 3, 1.5%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hypercalcemia grade 3, 2%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hyperglycemia grade 3, 2.1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Hypophosphatemia grade 3, 3.5%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Decreased hemoglobin grade 3, 3.7%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Lymphocyte count decreased grade 3, 8.3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Neutrophil count decreased grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Platelets decreased grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
WBC decreased grade 3, <1%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 54 years
Health Status: unhealthy
Age Group: median age was 54 years
Sex: M+F
Sources:
Arthralgia grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Nausea grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Photosensitivity reaction grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Rash grade 3, 3%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Squamous cell carcinoma, keratoacanthoma-type grade 3, 31%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Fatigue grade 3, 6%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Palmar-plantar erythrodysesthesia syndrome grade 3, 6%
960 mg 2 times / day multiple, oral
Recommended|MTD
Dose: 960 mg, 2 times / day
Route: oral
Route: multiple
Dose: 960 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Lymphopenia grade 3, 17%
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Pruritus grade 3, 17%
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Arthralgia grade 3, 17%
DLT
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Fatigue grade 3, 33%
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Squamous cell carcinoma, keratoacanthoma-type grade 3, 33%
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Rash grade 3, 50%
DLT
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Squamous cell carcinoma, keratoacanthoma-type grade 3, 50%
240 mg 2 times / day multiple, oral
Dose: 240 mg, 2 times / day
Route: oral
Route: multiple
Dose: 240 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Squamous cell carcinoma, keratoacanthoma-type grade 3, 38%
360 mg 2 times / day multiple, oral
Dose: 360 mg, 2 times / day
Route: oral
Route: multiple
Dose: 360 mg, 2 times / day
Sources:
unhealthy, median age was 63 years
Health Status: unhealthy
Age Group: median age was 63 years
Sex: M+F
Sources:
Fatigue 60%
DLT
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy
Rash 60%
DLT
1120 mg 2 times / day multiple, oral
Dose: 1120 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1120 mg, 2 times / day
Sources:
unhealthy
ALT increased grade 3
360 mg 2 times / day multiple, oral
Dose: 360 mg, 2 times / day
Route: oral
Route: multiple
Dose: 360 mg, 2 times / day
Sources:
unhealthy
Pancytopenia grade 4
DLT
720 mg 2 times / day multiple, oral
Dose: 720 mg, 2 times / day
Route: oral
Route: multiple
Dose: 720 mg, 2 times / day
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
mild [IC50 33.2 uM]
yes (co-administration study)
Comment: Vemurafenib increased the AUC0-last of the CYP2D6 substrate (dextromethorphan) by 47%, and therefore can be classified as a weak inhibitor of CYP2D6 based on the FDA guidance.
Page: -
moderate [IC50 32.5 uM]
yes (co-administration study)
Comment: Сoadministration of vemurafenib increased the AUC0-last of caffeine (CYP1A2 substrate) by 2.6-fold
Page: -
no
no
yes [IC50 22.5 uM]
yes [IC50 5.9 uM]
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: Сoadministration of vemurafenib decreased the AUC0-last of midazolam (CYP3A4 substrate) by 39%,
Page: -
Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas.
2010 Dec
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.
2010 Sep 30
The BRAFT1799A mutation confers sensitivity of thyroid cancer cells to the BRAFV600E inhibitor PLX4032 (RG7204).
2011 Jan 28
Novel immunotherapeutic agents and small molecule antagonists of signalling kinases for the treatment of metastatic melanoma.
2011 Jul 9
Improved survival with vemurafenib in melanoma with BRAF V600E mutation.
2011 Jun 30
Overcoming metastatic melanoma with BRAF inhibitors.
2011 May
BRAF targeted therapy changes the treatment paradigm in melanoma.
2011 May 24
Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells.
2015 Aug 18
The quinone methide aurin is a heat shock response inducer that causes proteotoxic stress and Noxa-dependent apoptosis in malignant melanoma cells.
2015 Jan 16
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.
2015 May 18
Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
2015 Sep 14
Patents

Sample Use Guides

960 mg twice daily. Administer ZELBORAF approximately 12 hours apart with or without a meal. Management of symptomatic adverse drug reactions may require dose reduction, treatment interruption, or treatment discontinuation of ZELBORAF. Dose reductions resulting in a dose below 480 mg twice daily are not recommended
Route of Administration: Oral
The antitumor effects of vemurafenib against SM1 cells were tested by in vitro MTS cell proliferation assay after 72 hours of treatment. The IC50 of vemurafenib was 14 uM, which is approximately one log higher than the sensitivity of M229 (IC50 of 0.5 uM), a BRAF V600E mutant human melanoma cell line highly sensitive to vemurafenib, and at a similar range as the relatively resistant BRAF V600E mutant human melanoma cell line M233 (IC50 of 15 uM).
Substance Class Chemical
Created
by admin
on Mon Mar 31 19:14:41 GMT 2025
Edited
by admin
on Mon Mar 31 19:14:41 GMT 2025
Record UNII
207SMY3FQT
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
vemurafenib [INN]
Preferred Name English
VEMURAFENIB
DASH   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
RG 7204
Code English
VEMURAFENIB [ORANGE BOOK]
Common Name English
ZELBORAF
Brand Name English
N-(3-((5-(4-CHLOROPHENYL)-1H-PYRROLO(2,3-B)PYRIDIN-3-YL)CARBONYL)-2,4- DIFLUOROPHENYL)PROPANE-1-SULFONAMIDE
Systematic Name English
VEMURAFENIB [VANDF]
Common Name English
RO-51-85426
Code English
VEMURAFENIB [MART.]
Common Name English
VEMURAFENIB [USAN]
Common Name English
PLX-4032
Code English
RO 5185426
Code English
RO-5185426
Code English
VEMURAFENIB [JAN]
Common Name English
Vemurafenib [WHO-DD]
Common Name English
1-PROPANESULFONAMIDE, N-(3-((5-(4-CHLOROPHENYL)-1H-PYRROLO(2,3-B)PYRIDIN-3- YL)CARBONYL)-2,4-DIFLUOROPHENYL)-
Systematic Name English
VEMURAFENIB [MI]
Common Name English
PLX4032
Code English
RG-7204
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 325310
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
FDA ORPHAN DRUG 444114
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
EMA ASSESSMENT REPORTS ZELBORAF (AUTHORIZED: MELANOMA)
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
EU-Orphan Drug EU/3/17/1846
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
FDA ORPHAN DRUG 444314
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
NDF-RT N0000175605
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
WHO-VATC QL01XE15
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
LIVERTOX NBK548656
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
FDA ORPHAN DRUG 529616
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
FDA ORPHAN DRUG 399213
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
NCI_THESAURUS C2189
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
WHO-ATC L01XE15
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
Code System Code Type Description
IUPHAR
5893
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
RXCUI
1147220
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY RxNorm
EVMPD
SUB32161
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
NDF-RT
N0000185503
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY P-Glycoprotein Inhibitors [MoA]
PUBCHEM
42611257
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
MERCK INDEX
m11408
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY Merck Index
DRUG CENTRAL
4185
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
CHEBI
63637
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
INN
9286
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
NCI_THESAURUS
C64768
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
LACTMED
Vemurafenib
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
ChEMBL
CHEMBL1229517
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
FDA UNII
207SMY3FQT
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
MESH
C551177
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
CAS
918504-65-1
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
HSDB
8143
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
EPA CompTox
DTXSID50238710
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
USAN
YY-42
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
DAILYMED
207SMY3FQT
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
DRUG BANK
DB08881
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
NDF-RT
N0000182138
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY Cytochrome P450 1A2 Inhibitors [MoA]
SMS_ID
100000124528
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
WIKIPEDIA
VEMURAFENIB
Created by admin on Mon Mar 31 19:14:41 GMT 2025 , Edited by admin on Mon Mar 31 19:14:41 GMT 2025
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
From the human mass balance trial (NP25158), the mean percent of 14 C-vemurafenib related material recovered in feces and urine within 432 hrs pos t-dose was 94.1% and 0.97%, respectively.
FECAL
TRANSPORTER -> INHIBITOR
MDCKII- MDR1 cells.
IC50
TARGET -> INHIBITOR
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
From the human mass balance trial (NP25158), the mean percent of 14 C-vemurafenib related material recovered in feces and urine within 432 hrs pos t-dose was 94.1% and 0.97%, respectively.
URINE
LABELED -> NON-LABELED
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
COMPETITIVE INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
MDCKII- MDR1 cells.
IC50
Related Record Type Details
ACTIVE MOIETY
FECAL; URINE
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC