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
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)
Molecular Formula | C23H20F3N5O2S2 |
Molecular Weight | 519.562 |
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
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=23249624
Curator's Comment: Dabrafenib crosses blood-brain barrier and has anticancer activity in the CNS
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P15056|||Q13878 Gene ID: 673.0 Gene Symbol: BRAF Target Organism: Homo sapiens (Human) |
3.2 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | TAFINLAR Approved UseIndicated 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 Date2013 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
806 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22608338/ |
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: UNKNOWN |
|
2497.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29399853/ |
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4341 ng × 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 |
|
2619 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22608338/ |
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: UNKNOWN |
|
13485.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29399853/ |
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
5.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22608338/ |
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: UNKNOWN |
|
4.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29399853/ |
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 |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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) Sources: Hepatic pain (serious, 1 patient) Myocardial infarction (serious, 1 patient) Tricuspid valve disease (2 patients) Muscular weakness (serious, 2 patients) |
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%) Sources: Hyperkeratosis (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 (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%) Sources: 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%) |
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%) Sources: Malaise (1%) Small intestinal perforation (1%) Neutropenia (1%) Thrombocytopenia (1%) Cataract (1%) Gastrointestinal infection (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 (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%) Sources: Muscle spasms (1%) Musculoskeletal stiffness (1%) Pemphigoid (1%) Hyperkeratosis (1%) Urinary bladder polyp (1%) Urinary retention (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: |
Disc. AE: Pyrexia, Pyrexia... AEs leading to discontinuation/dose reduction: Pyrexia (all grades, 28%) Sources: Pyrexia (grade 3-4, 3%) Fatigue (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: |
Disc. AE: Back pain, Back pain... AEs leading to discontinuation/dose reduction: Back pain (all grades, 12%) Sources: Back pain (grade 3-4, 3%) Myalgia (all grades, 11%) |
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: Constipation, Constipation... AEs leading to discontinuation/dose reduction: Constipation (all grades, 11%) Sources: Constipation (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: |
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%) Other AEs: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%) Hyperkeratosis (all grades, 37%) Sources: 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%) |
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 |
Other AEs: Squamous cell carcinoma of skin, Pyrexia... Other AEs: Squamous cell carcinoma of skin (grade 3, 25%) Sources: Pyrexia (grade 2, 5%) |
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 |
DLT: Hyponatraemia, Squamous cell carcinoma of skin... Dose limiting toxicities: Hyponatraemia (grade 4, 1 patient) Sources: Squamous cell carcinoma of skin (grade 3, 1 patient) |
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 Health Status: unhealthy Sources: |
Disc. AE: Pancytopenia, Lymphocytopenia... AEs leading to discontinuation/dose reduction: Pancytopenia (2 patients) Sources: 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) |
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 |
DLT: Squamous cell carcinoma of skin, Syncope... Dose limiting toxicities: Squamous cell carcinoma of skin (grade 3, 1 patient) Sources: Syncope (grade 3, 1 patient) Pyrexia (grade 2, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
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: |
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: |
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: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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: |
unhealthy, 53 years Health Status: unhealthy Age Group: 53 years Sex: M+F Sources: |
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 |
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 |
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 |
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 |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 |
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 |
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=26 Page: - |
|||
yes [IC50 8.2 uM] | ||||
yes [IC50 87 uM] | unlikely Comment: [I]/Ki=0.07 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=27 Page: - |
|||
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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=10 Page: - |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=10 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=10 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/202806Orig1s000ClinPharmR.pdf#page=27 Page: - |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
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
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=26497853
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
Edited
Mon Mar 31 20:25:00 GMT 2025
by
admin
on
Mon Mar 31 20:25:00 GMT 2025
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Record UNII |
QGP4HA4G1B
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Record Status |
Validated (UNII)
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Record Version |
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-
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Official Name | English | ||
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Preferred Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Code | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Systematic Name | English |
Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
775820
Created by
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FDA ORPHAN DRUG |
521616
Created by
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WHO-ATC |
L01XE23
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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NCI_THESAURUS |
C155322
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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FDA ORPHAN DRUG |
495915
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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NCI_THESAURUS |
C129825
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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EMA ASSESSMENT REPORTS |
TAFINLAR (AUTHORIZED: MELANOMA)
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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WHO-VATC |
QL01XE23
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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FDA ORPHAN DRUG |
376812
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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FDA ORPHAN DRUG |
329610
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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FDA ORPHAN DRUG |
448214
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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FDA ORPHAN DRUG |
506415
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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NDF-RT |
N0000175605
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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N0000190108
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Organic Anion Transporting Polypeptide 1B3 Inhibitors [MoA] | ||
|
m11719
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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1195765-45-7
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
|
N0000185506
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Cytochrome P450 3A4 Inducers [MoA] | ||
|
75045
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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N0000190107
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA] | ||
|
CHEMBL2028663
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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N0000185507
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Cytochrome P450 2C9 Inducers [MoA] | ||
|
SUB45696
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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4801
Created by
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PRIMARY | |||
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9458
Created by
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PRIMARY | |||
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N0000185607
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Cytochrome P450 2C19 Inducers [MoA] | ||
|
N0000187064
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Cytochrome P450 2B6 Inducers [MoA] | ||
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44462760
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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N0000190110
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Organic Anion Transporter 1 Inhibitors [MoA] | ||
|
6494
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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QGP4HA4G1B
Created by
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PRIMARY | |||
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DB08912
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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100000131505
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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N0000187063
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Cytochrome P450 2C8 Inducers [MoA] | ||
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C82386
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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Dabrafenib
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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N0000190113
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Breast Cancer Resistance Protein Inhibitors [MoA] | ||
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DTXSID20152499
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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Dabrafenib
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | |||
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1424911
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | RxNorm | ||
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QGP4HA4G1B
Created by
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PRIMARY | |||
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N0000190111
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY | Organic Anion Transporter 3 Inhibitors [MoA] | ||
|
XX-156
Created by
admin on Mon Mar 31 20:25:00 GMT 2025 , Edited by admin on Mon Mar 31 20:25:00 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR |
IC50
|
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SALT/SOLVATE -> PARENT |
|
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TARGET -> INHIBITOR |
An ATP competitive inhibitor.
COMPETITIVE INHIBITOR
IC50
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|
TARGET -> INHIBITOR |
An ATP competitive inhibitor. Binding assay
COMPETITIVE INHIBITOR
IC50
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TRANSPORTER -> INHIBITOR |
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> NON-INHIBITOR |
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TRANSPORTER -> INHIBITOR |
[i}/IC50= 2.03; CMAX=2.84
IC50
|
||
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METABOLIC ENZYME -> SUBSTRATE |
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TARGET -> INHIBITOR |
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METABOLIC ENZYME -> INDUCER |
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
URINE
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METABOLITE ACTIVE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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