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
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)
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 |
DescriptionCurator'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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=24353011
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
Sources: http://www.webmd.com/melanoma-skin-cancer/news/20110817/zelboraf-approved-for-late-stage-melanoma
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5145 |
31.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | ZELBORAF Approved UseIndicated 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 Date2011 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
52.7 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3127.1 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
34.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24178368 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse events |
---|---|---|
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, Photosensitivity reaction... Other AEs: Rash (grade 3, 8%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Other AEs:Rash (grade 3, 50%) Squamous cell carcinoma, keratoacanthoma-type (grade 3, 33%) Sources: Fatigue (grade 3, 33%) Pruritus (grade 3, 17%) Lymphopenia (grade 3, 17%) |
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%) Sources: Fatigue (60%) |
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
AE | Significance | Dose | Population |
---|---|---|---|
Seborrheic keratosis | 10% | 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: |
Sunburn | 10% | 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: |
Asthenia | 11% | 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: |
Constipation | 12% | 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: |
Myalgia | 13% | 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: |
Dysgeusia | 14% | 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: |
Erythema | 14% | 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: |
Edema peripheral | 17% | 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 appetite | 18% | 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 | 18% | 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 | 18% | 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: |
Dry skin | 19% | 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: |
Pyrexia | 19% | 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: |
Skin papilloma | 21% | 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: |
Headache | 23% | 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 | 23% | 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 | 24% | 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: |
Squamous cell carcinoma of skin | 24% | 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: |
Diarrhea | 28% | 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 | 33% | 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 | 35% | 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 | 37% | 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 | 38% | 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: |
Alopecia | 45% | 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 | 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 papular | 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: |
Arthralgia | 53% | 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: |
Actinic keratosis | 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: |
Back pain | 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: |
Cough | 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: |
Musculoskeletal pain | 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: |
Rash maculo-papular | 9% | 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% | 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% | 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% | 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% | 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% | 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 maculo-papular | 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: |
Squamous cell carcinoma of skin | grade 3, 22% | 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% | 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, 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% | 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% | 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: |
Alopecia | 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: |
Asthenia | 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: |
Back pain | 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: |
Constipation | 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: |
Diarrhea | 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: |
Edema peripheral | 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: |
Headache | 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: |
Myalgia | 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: |
Pain in extremity | 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: |
Pyrexia | 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: |
Rash papular | 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: |
Seborrheic keratosis | 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: |
Skin papilloma | 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: |
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202429Orig1s000ClinPharmR.pdf#page=16 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202429Orig1s000ClinPharmR.pdf#page=16 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%, Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202429Orig1s000ClinPharmR.pdf#page=16 Page: - |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=22693252
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
Edited
Mon Mar 31 19:14:41 GMT 2025
by
admin
on
Mon Mar 31 19:14:41 GMT 2025
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Record UNII |
207SMY3FQT
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Record Status |
Validated (UNII)
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Record Version |
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Code | English | ||
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Common Name | English | ||
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Code | English |
Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
325310
Created by
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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
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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
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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
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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
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FDA ORPHAN DRUG |
444314
Created by
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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
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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
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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
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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
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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
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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
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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
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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5893
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PRIMARY | |||
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1147220
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PRIMARY | RxNorm | ||
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SUB32161
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PRIMARY | |||
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N0000185503
Created by
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
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42611257
Created by
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PRIMARY | |||
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m11408
Created by
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PRIMARY | Merck Index | ||
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4185
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PRIMARY | |||
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63637
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PRIMARY | |||
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9286
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PRIMARY | |||
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C64768
Created by
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PRIMARY | |||
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Vemurafenib
Created by
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PRIMARY | |||
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CHEMBL1229517
Created by
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PRIMARY | |||
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207SMY3FQT
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PRIMARY | |||
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C551177
Created by
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PRIMARY | |||
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918504-65-1
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PRIMARY | |||
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8143
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PRIMARY | |||
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DTXSID50238710
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PRIMARY | |||
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YY-42
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PRIMARY | |||
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207SMY3FQT
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PRIMARY | |||
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DB08881
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PRIMARY | |||
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N0000182138
Created by
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PRIMARY | Cytochrome P450 1A2 Inhibitors [MoA] | ||
|
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
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PRIMARY | |||
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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
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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 |
|
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|
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
|
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|
LABELED -> NON-LABELED |
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|
TRANSPORTER -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
COMPETITIVE INHIBITOR
IC50
|
||
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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 |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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