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Details

Stereochemistry ACHIRAL
Molecular Formula C23H20F3N5O2S2
Molecular Weight 519.5654
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DABRAFENIB

SMILES

CC(C)(C)c1nc(-c2cccc(c2F)NS(=O)(=O)c3c(cccc3F)F)c(-c4cc[nH]c(=N)n4)s1

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

Molecular Formula C23H20F3N5O2S2
Molecular Weight 519.5654
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P15056|||Q13878
Gene ID: 673
Gene Symbol: BRAF
Target Organism: Homo sapiens (Human)
3.20000000000000018 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1369785600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2497.4 ng/mL
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
806 ng/mL
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
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
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2619 ng × h/mL
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
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
300 mg 2 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: TRAMETINIB
DABRAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.2 h
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
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%
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
Disc. AE: Pain, Hyperkeratosis...
AEs leading to
discontinuation/dose reduction:
Pain (1%)
Hyperkeratosis (1%)
Sources:
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Disc. AE: Constipation, Constipation...
AEs leading to
discontinuation/dose reduction:
Constipation (all grades, 11%)
Constipation (grade 3-4, 2%)
Sources:
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
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:
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Disc. AE: Pyrexia, Pyrexia...
AEs leading to
discontinuation/dose reduction:
Pyrexia (all grades, 28%)
Pyrexia (grade 3-4, 3%)
Fatigue (2%)
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
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:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Squamous cell carcinoma of skin, Pyrexia...
Other AEs:
Squamous cell carcinoma of skin (grade 3, 25%)
Pyrexia (grade 2, 5%)
Sources:
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
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:
unhealthy
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:
200 mg 2 times / day multiple, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
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:
unhealthy, 53 years (range: 22-93 years)
Health Status: unhealthy
Age Group: 53 years (range: 22-93 years)
Sex: M+F
Sources:
Constipation all grades, 11%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Constipation grade 3-4, 2%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Myalgia all grades, 11%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Back pain all grades, 12%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Back pain grade 3-4, 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Fatigue 2%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Pyrexia all grades, 28%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
Pyrexia grade 3-4, 3%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
unhealthy, 53 years
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy, 53 years
Health Status: unhealthy
Age Group: 53 years
Sex: M+F
Sources:
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:
unhealthy
Health Status: unhealthy
Sources:
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:
unhealthy
Health Status: unhealthy
Sources:
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
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:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
yes [IC50 1.4 uM]
yes [IC50 16 uM]
yes [IC50 22 uM]
yes [IC50 3.4 uM]
yes [IC50 4.7 uM]
yes [IC50 5.4 uM]
yes [IC50 6.9 uM]
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: -
yes [IC50 8.2 uM]
yes [IC50 87 uM]
yes
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
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: -
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: -
minor
minor
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

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

Sample Use Guides

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
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.
Substance Class Chemical
Created
by admin
on Sat Jun 26 15:47:22 UTC 2021
Edited
by admin
on Sat Jun 26 15:47:22 UTC 2021
Record UNII
QGP4HA4G1B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DABRAFENIB
DASH   INN   USAN   VANDF   WHO-DD  
USAN   INN  
Official 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
DABRAFENIB [WHO-DD]
Common 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 Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 521616
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
WHO-ATC L01XE23
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 506415
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
NCI_THESAURUS C155322
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 495915
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
EMA ASSESSMENT REPORTS TAFINLAR (AUTHORIZED: MELANOMA)
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
WHO-VATC QL01XE23
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 376812
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 329610
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
FDA ORPHAN DRUG 448214
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
Code System Code Type Description
NDF-RT
N0000190108
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B3 Inhibitors [MoA]
MERCK INDEX
M11719
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
CAS
1195765-45-7
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000185506
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
NDF-RT
N0000190107
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]
ChEMBL
CHEMBL2028663
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000185507
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Cytochrome P450 2C9 Inducers [MoA]
EVMPD
SUB45696
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
DRUG CENTRAL
4801
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
INN
9458
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000185607
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Cytochrome P450 2C19 Inducers [MoA]
NDF-RT
N0000187064
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Cytochrome P450 2B6 Inducers [MoA]
PUBCHEM
44462760
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000190110
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Organic Anion Transporter 1 Inhibitors [MoA]
IUPHAR
6494
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
FDA UNII
QGP4HA4G1B
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
DRUG BANK
DB08912
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000187063
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Cytochrome P450 2C8 Inducers [MoA]
NCI_THESAURUS
C82386
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
LACTMED
Dabrafenib
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
NDF-RT
N0000190113
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
EPA CompTox
1195765-45-7
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
WIKIPEDIA
Dabrafenib
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY
RXCUI
1424911
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY RxNorm
NDF-RT
N0000190111
Created by admin on Sat Jun 26 15:47:23 UTC 2021 , Edited by admin on Sat Jun 26 15:47:23 UTC 2021
PRIMARY Organic Anion Transporter 3 Inhibitors [MoA]
Related Record Type Details
TRANSPORTER -> INHIBITOR
IC50
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> INHIBITOR
BINDER->LIGAND
BINDING
TRANSPORTER -> NON-INHIBITOR
TRANSPORTER -> INHIBITOR
[i}/IC50= 2.03; CMAX=2.84
IC50
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
METABOLIC ENZYME -> INDUCER
Related Record Type Details
METABOLITE -> PARENT
URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC