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

Details

Stereochemistry ACHIRAL
Molecular Formula C23H20F3N5O2S2
Molecular Weight 519.562
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DABRAFENIB

SMILES

CC(C)(C)C1=NC(=C(S1)C2=NC(N)=NC=C2)C3=CC=CC(NS(=O)(=O)C4=C(F)C=CC=C4F)=C3F

InChI

InChIKey=BFSMGDJOXZAERB-UHFFFAOYSA-N
InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29)

HIDE SMILES / InChI

Description

Dabrafenib is a selective, orally bioavailable inhibitor of Mutant BRAF protein kinase with potential antineoplastic activity. Dabrafenib inhibits BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM. BRAF belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. Mutations in BRAF are associated with increased growth and proliferation of cancer cells. By inhibiting BRAF kinase dabrafenib negatively regulates the proliferation of tumor cells which contain a mutated BRAF gene. Dabrafenib (in combination with trametinib or alone) is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E mutation

CNS Activity

CNS Active
3913
Curator's Comment: Dabrafenib crosses blood-brain barrier and has anticancer activity in the CNS

Originator

Approval Year

2013
596
Targets

Targets

Primary TargetPharmacologyConditionPotency
Serine/threonine-protein kinase B-raf
20
Target ID: P15056|||Q13878
Gene ID: 673.0
Gene Symbol: BRAF
Target Organism: Homo sapiens (Human)
Inhibitor
8297
 3.2 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
TAFINLAR

Approved Use

Indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test; in combination with trametinib, for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. Limitation of Use: TAFINLAR is not indicated for treatment of patients with wild-type BRAF melanoma.

Launch Date

2013
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2497.4 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5947742/pdf/JDE-45-397.pdf
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
TRAMETINIB
 DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
806 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1478 ng/mL
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/tafinlar-epar-product-information_en.pdf
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
13485.6 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5947742/pdf/JDE-45-397.pdf
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
TRAMETINIB
 DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2619 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4341 μg × h/mL
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/tafinlar-epar-product-information_en.pdf
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.9 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5947742/pdf/JDE-45-397.pdf
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
TRAMETINIB
 DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.2 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8 h
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/tafinlar-epar-product-information_en.pdf
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.3%
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/tafinlar-epar-product-information_en.pdf
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Disc. AE: Constipation, Hepatic pain...
AEs leading to
discontinuation/dose reduction:
Constipation (serious, 1 patient)
Hepatic pain (serious, 1 patient)
Myocardial infarction (serious, 1 patient)
Tricuspid valve disease (2 patients)
Muscular weakness (serious, 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
Disc. AE: Pain, Hyperkeratosis...
AEs leading to
discontinuation/dose reduction:
Pain (1%)
Hyperkeratosis (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Disc. AE: Hyperhidrosis, Migraine...
AEs leading to
discontinuation/dose reduction:
Hyperhidrosis (1%)
Migraine (1%)
Syncope (1%)
Vomiting (1%)
Diarrhea (1%)
Nausea (1%)
Atrial fibrillation (1%)
Alanine aminotransferase increased (1%)
Aspartate aminotransferase increased (1%)
Diabetes mellitus (1%)
Diabetes mellitus inadequate control (1%)
Pulmonary edema (1%)
Respiratory distress (1%)
Pleural effusion (1%)
Alkaline phosphatase increased (1%)
Ejection fraction decreased (1%)
Gamma-glutamyltransferase increased (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Disc. AE: Oropharyngeal pain, Malaise...
AEs leading to
discontinuation/dose reduction:
Oropharyngeal pain (1%)
Malaise (1%)
Small intestinal perforation (1%)
Neutropenia (1%)
Thrombocytopenia (1%)
Cataract (1%)
Gastrointestinal infection (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Disc. AE: Back pain, Muscle spasms...
AEs leading to
discontinuation/dose reduction:
Back pain (1%)
Muscle spasms (1%)
Musculoskeletal stiffness (1%)
Pemphigoid (1%)
Hyperkeratosis (1%)
Urinary bladder polyp (1%)
Urinary retention (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Disc. AE: Pyrexia, Pyrexia...
AEs leading to
discontinuation/dose reduction:
Pyrexia (all grades, 28%)
Pyrexia (grade 3-4, 3%)
Fatigue (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Disc. AE: Constipation, Constipation...
AEs leading to
discontinuation/dose reduction:
Constipation (all grades, 11%)
Constipation (grade 3-4, 2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Disc. AE: Back pain, Back pain...
AEs leading to
discontinuation/dose reduction:
Back pain (all grades, 12%)
Back pain (grade 3-4, 3%)
Myalgia (all grades, 11%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Disc. AE: Squamous cell carcinoma of skin, Keratoacanthoma...
Other AEs: Hyperkeratosis, Hyperkeratosis...
AEs leading to
discontinuation/dose reduction:
Squamous cell carcinoma of skin (grade 3-4, 4%)
Keratoacanthoma (grade 3-4, 4%)
Headache (all grades, 32%)
Arthralgia (all grades, 27%)
Arthralgia (grade 3-4, 1%)
Chills (3%)
Palmar-plantar erythrodysesthesia syndrome (3%)
Hypophosphatemia (37%)
Hypophosphatemia (6%)
Pancreatitis (<10%)
Other AEs:
Hyperkeratosis (all grades, 37%)
Hyperkeratosis (grade 3-4, 1%)
Alopecia (all grades, 22%)
Palmar-plantar erythrodysesthesia syndrome (all grades, 20%)
Palmar-plantar erythrodysesthesia syndrome (grade 3-4, 2%)
Rash (all grades, 17%)
Papilloma (all grades, 27%)
Cough (all grades, 12%)
Nasopharyngitis (all grades, 10%)
Hyperglycemia (all grades, 50%)
Hyperglycemia (grade 3-4, 6%)
Alkaline phosphatase increased (19%)
Hyponatremia (8%)
Hyponatremia (2%)
Bullous rash (<10%)
Nephritis interstitial (<10%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
100 mg 3 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
unhealthy
n = 20
Health Status: unhealthy
Population Size: 20
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
Other AEs: Squamous cell carcinoma of skin, Pyrexia...
Other AEs:
Squamous cell carcinoma of skin (grade 3, 25%)
Pyrexia (grade 2, 5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 10
Health Status: unhealthy
Sex: M+F
Population Size: 10
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
DLT: Hyponatraemia, Squamous cell carcinoma of skin...
Dose limiting toxicities:
Hyponatraemia (grade 4, 1 patient)
Squamous cell carcinoma of skin (grade 3, 1 patient)
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Disc. AE: Pancytopenia, Lymphocytopenia...
AEs leading to
discontinuation/dose reduction:
Pancytopenia (2 patients)
Lymphocytopenia (1 patient)
Infarct myocardial (grade 5, 1 patient)
Acute coronary syndrome (grade 5, 1 patient)
Heart attack (1 patient)
Abdominal pain (severe, 1 patient)
Glissonitis (1 patient)
Creatinine increased (1 patient)
Epileptic seizure (1 patient)
Cerebral hemorrhage (grade 5, 1 patient)
Hyponatremia (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
200 mg 2 times / day multiple, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 20
Health Status: unhealthy
Sex: M+F
Population Size: 20
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
DLT: Squamous cell carcinoma of skin, Syncope...
Dose limiting toxicities:
Squamous cell carcinoma of skin (grade 3, 1 patient)
Syncope (grade 3, 1 patient)
Pyrexia (grade 2, 1 patient)
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
AEs

AEs

AESignificanceDosePopulation
Tricuspid valve disease 2 patients
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Constipation serious, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Hepatic pain serious, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Myocardial infarction serious, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Muscular weakness serious, 2 patients
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 94
Hyperkeratosis 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
Pain 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 96
Alanine aminotransferase increased 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Alkaline phosphatase increased 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Aspartate aminotransferase increased 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Atrial fibrillation 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Diabetes mellitus inadequate control 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Diabetes mellitus 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Diarrhea 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Ejection fraction decreased 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Gamma-glutamyltransferase increased 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Hyperhidrosis 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Migraine 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Nausea 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Pleural effusion 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Pulmonary edema 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Respiratory distress 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Syncope 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Vomiting 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 97
Cataract 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Gastrointestinal infection 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Malaise 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Neutropenia 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Oropharyngeal pain 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Small intestinal perforation 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Thrombocytopenia 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 98
Back pain 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Hyperkeratosis 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Muscle spasms 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Musculoskeletal stiffness 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Pemphigoid 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Urinary bladder polyp 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Urinary retention 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
unhealthy, 53 years (range: 22-93 years)
n = 187
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 99
Fatigue 2%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Pyrexia all grades, 28%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Pyrexia grade 3-4, 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Constipation all grades, 11%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Constipation grade 3-4, 2%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Myalgia all grades, 11%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Back pain all grades, 12%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Back pain grade 3-4, 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Alkaline phosphatase increased 19%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyponatremia 2%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Chills 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Palmar-plantar erythrodysesthesia syndrome 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hypophosphatemia 37%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hypophosphatemia 6%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyponatremia 8%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Bullous rash <10%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Nephritis interstitial <10%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Pancreatitis <10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Nasopharyngitis all grades, 10%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Cough all grades, 12%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Rash all grades, 17%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Palmar-plantar erythrodysesthesia syndrome all grades, 20%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Alopecia all grades, 22%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Papilloma all grades, 27%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Arthralgia all grades, 27%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Headache all grades, 32%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyperkeratosis all grades, 37%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyperglycemia all grades, 50%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyperkeratosis grade 3-4, 1%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Arthralgia grade 3-4, 1%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Palmar-plantar erythrodysesthesia syndrome grade 3-4, 2%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Keratoacanthoma grade 3-4, 4%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Squamous cell carcinoma of skin grade 3-4, 4%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Hyperglycemia grade 3-4, 6%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
unhealthy, 53 years
n = 187
Health Status: unhealthy
Condition: unresectable or metastatic melanoma with BRAF V600E mutation-positive melanoma
Age Group: 53 years
Sex: M+F
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202806s000lbl.pdf
Pyrexia grade 2, 5%
100 mg 3 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
unhealthy
n = 20
Health Status: unhealthy
Population Size: 20
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
Squamous cell carcinoma of skin grade 3, 25%
100 mg 3 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
unhealthy
n = 20
Health Status: unhealthy
Population Size: 20
Sources:
https://pubmed.ncbi.nlm.nih.gov/24958809
Squamous cell carcinoma of skin grade 3, 1 patient
DLT
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 10
Health Status: unhealthy
Sex: M+F
Population Size: 10
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
Hyponatraemia grade 4, 1 patient
DLT
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 10
Health Status: unhealthy
Sex: M+F
Population Size: 10
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
Creatinine increased 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Epileptic seizure 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Glissonitis 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Heart attack 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Hyponatremia 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Lymphocytopenia 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Pancytopenia 2 patients
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Acute coronary syndrome grade 5, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Cerebral hemorrhage grade 5, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Infarct myocardial grade 5, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Abdominal pain severe, 1 patient
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
unhealthy
n = 187
Health Status: unhealthy
Population Size: 187
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000MedR.pdf
Page: p. 95
Pyrexia grade 2, 1 patient
DLT
200 mg 2 times / day multiple, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 20
Health Status: unhealthy
Sex: M+F
Population Size: 20
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
Squamous cell carcinoma of skin grade 3, 1 patient
DLT
200 mg 2 times / day multiple, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 20
Health Status: unhealthy
Sex: M+F
Population Size: 20
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
Syncope grade 3, 1 patient
DLT
200 mg 2 times / day multiple, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
unhealthy
n = 20
Health Status: unhealthy
Sex: M+F
Population Size: 20
Sources:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109288/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inducer
781

inhibitor
1587
substrate
1037

inhibitor
1767
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
911

CYP2C19
1478

CYP1A2
1524

BCRP
699

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

P-gp
1461
CYP2C8
693

CYP2C19
991

P-gp
1537
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
P-gp
1650
 no
OATP1B1
803
 yes [IC50 1.4 uM]
CYP3A4
1925
 yes [IC50 16 uM]
CYP2C19
1553
 yes [IC50 22 uM]
OAT3
644
 yes [IC50 3.4 uM]
OATP1B3
715
 yes [IC50 4.7 uM]
BCRP
773
 yes [IC50 5.4 uM]
OAT1
603
 yes [IC50 6.9 uM]
CYP2C9
1819
 yes [IC50 7.2 uM]
unknown (co-administration study)
Comment: A study (BRF113771, Part A) of the effect of repeat dose dabrafenib on single dose warfarin, a CYP2C9 substrate, is ongoing. This study will provide a more definitive assessment of the inhibitory or induction risk of dabrafenib on a CYP2C9 substrate (warfarin).
Page: -
CYP2C8
965
 yes [IC50 8.2 uM]
CYP1A2
1692
 yes [IC50 87 uM]
CYP2B6
1001
 yes
CYP3A4
1925
 yes
yes (co-administration study)
Comment: A decrease in single dose midazolam CIliax and AUQo-oo) was observed with repeat dosing of dabrafenib 150 mg BID. with a mean ratio (90% CI) of 0.39 (0.24, 0.63) for Cm, and 0.26 (0.21, 0.32) for AUC(o-oo), indicating that dabrafenib induces CYP3A4-mediated metabolism (Table 12). Based on this result, dabrafenib appears to be a moderate inducer of CYP3A4 in vivo.. The effect of dabrafenib on dexamethasone, a CYP3A4 substrate, was planned as part of Study BRF113929, but subjects for that cohort could not be recruited. PK data in the only 2 subjects enrolled showed a decrease in dexamethasone concentrations with dabrafenib, consistent with CYP3A4 induction.
Page: -
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C8
693
 major
unknown (co-administration study)
Comment: The effects of strong inhibitors or inducers of CYP3A4 or CYP2C8 on pharmacokinetics of dabrafenib in vivo are to be studied under PMRs.
Page: -
CYP3A4
1737
 major
yes (co-administration study)
Comment: A decrease in single-dose midazolam exposure with mean (90% CI) ratios of 0.39 (0.25, 0.63) for Cmax and 0.26 (0.21, 0.32) for AUC, respectively, was observed with repeat dosing of dabrafenib 150 mg BID, indicating that dabrafenib induces CYP3A4-mediated metabolism.
Page: -
CYP2C19
991
 minor
CYP2C9
1037
 minor
P-gp
1537
 yes
unlikely
Comment: Given the high oral bioavailability (94.5%) and high metabolic clearance, these efflux transporters appear to have minimal impact on bioavailability and contribution to the parent drug elimination. The potential impact of Pgp and/or BCRP inhibitors on the elimination of dabrafenib is considered low.
Page: -
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:75045
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:75045
ChemicalBook
CB32604230
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32604230
MolPort
MolPort-028-720-422
https://www.molport.com/shop/molecule-link/MolPort-028-720-422
Selleck Chemicals
dabrafenib-gsk2118436a
http://www.selleckchem.com/products/dabrafenib-gsk2118436a.html
ZINC
ZINC000068153186
http://zinc15.docking.org/substances/ZINC000068153186
eMolecules
36008941
https://www.emolecules.com/cgi-bin/more?vid=36008941
PubMed

PubMed

TitleDatePubMed
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.
2010 Sep 30
Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies.
2013 Jul
BRAF inhibitor activity in V600R metastatic melanoma.
2013 Mar
Patents

Patents

07994185
12
08415345
12
08642759
5
08703781
2
20090298815
6
JP2013537228A
5

Sample Use Guides

In Vivo Use Guide
The recommended dosage regimens are: 150 mg orally taken twice daily, approximately 12 hours apart, as a single agent or 150 mg orally taken twice daily, approximately 12 hours apart, in combination with trametinib 2 mg orally taken once daily.
Route of Administration: Oral
In Vitro Use Guide
A375, SK-MEL-28, WM239 and SK-MEL-5 cells with 2.5, 5 and 10 nM dabrafenib for 72 hours. Dabrafenib treatment induced massive Mcl-1 expression at all the three concentrations. The IC50 of dabrafenib in A375, SK-MEL-28 and WM-239 was 5nM, 2nM and 6nM respectively. In dabrafenib resistant A375, SK-MEL-28 and WM-239 cells, which were denoted as A375-DR, SK-MEL-28-DR and WM-239-DR that were incubated with up to 300 nM inhibitor concentrations the IC50s were greater than 100 nM indicating more than 30-fold resistance.
Name Type Language
DABRAFENIB
DASH   INN   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
Dabrafenib [WHO-DD]
Common Name English
GSK-2118436A
Code English
DABRAFENIB [MI]
Common Name English
GSK2118436A
Code English
GSK2118436
Common Name English
GSK-2118436
Code English
DABRAFENIB [USAN]
Common Name English
DABRAFENIB [VANDF]
Common Name English
BENZENESULFONAMIDE, N-(3-(5-(2-AMINO-4-PYRIMIDINYL)-2-(1,1-DIMETHYLETHYL)-4-THIAZOLYL)-2-FLUOROPHENYL)-2,6-DIFLUORO-
Systematic Name English
N-(3-(5-(2-AMINOPYRIMIDIN-4-YL)-2-TERT-BUTYL-1,3-THIAZOL-4-YL)-2-FLUOROPHENYL)-2,6-DIFLUOROBENZENESULFONAMIDE
Systematic Name English
dabrafenib [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 775820
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 521616
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
WHO-ATC L01XE23
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
NCI_THESAURUS C155322
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 495915
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
NCI_THESAURUS C129825
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
EMA ASSESSMENT REPORTS TAFINLAR (AUTHORIZED: MELANOMA)
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
WHO-VATC QL01XE23
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 376812
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 329610
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 448214
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
FDA ORPHAN DRUG 506415
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
NDF-RT N0000175605
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
Code System Code Type Description
NDF-RT
N0000190108
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Organic Anion Transporting Polypeptide 1B3 Inhibitors [MoA]
MERCK INDEX
m11719
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
CAS
1195765-45-7
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000185506
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
CHEBI
75045
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000190107
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]
ChEMBL
CHEMBL2028663
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000185507
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Cytochrome P450 2C9 Inducers [MoA]
EVMPD
SUB45696
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
DRUG CENTRAL
4801
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
INN
9458
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000185607
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Cytochrome P450 2C19 Inducers [MoA]
NDF-RT
N0000187064
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Cytochrome P450 2B6 Inducers [MoA]
PUBCHEM
44462760
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000190110
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Organic Anion Transporter 1 Inhibitors [MoA]
IUPHAR
6494
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
FDA UNII
QGP4HA4G1B
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
DRUG BANK
DB08912
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
SMS_ID
100000131505
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000187063
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Cytochrome P450 2C8 Inducers [MoA]
NCI_THESAURUS
C82386
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
LACTMED
Dabrafenib
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000190113
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
EPA CompTox
DTXSID20152499
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
WIKIPEDIA
Dabrafenib
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
RXCUI
1424911
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY RxNorm
DAILYMED
QGP4HA4G1B
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
NDF-RT
N0000190111
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY Organic Anion Transporter 3 Inhibitors [MoA]
USAN
XX-156
Created by admin on Fri Dec 15 22:10:35 GMT 2023 , Edited by admin on Fri Dec 15 22:10:35 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of DABRAFENIB
METABOLITE (PARENT)
Structure of CARBOXY DARAFENIB
METABOLITE ACTIVE (PARENT)
Structure of DESMETHYL DABRAFENIB
SALT/SOLVATE (PARENT)
Structure of DABRAFENIB MESYLATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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