Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C29H39ClN7O2P |
| Molecular Weight | 584.092 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(NC2=NC=C(Cl)C(NC3=CC=CC=C3P(C)(C)=O)=N2)C=CC(=C1)N4CCC(CC4)N5CCN(C)CC5
InChI
InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N
InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34)
| Molecular Formula | C29H39ClN7O2P |
| Molecular Weight | 584.092 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27780853
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27780853
Brigatinib (AP26113) is an investigational, targeted cancer medicine discovered internally at ARIAD Pharmaceuticals, Inc. Brigatinib has exhibited activity as a potent dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). It is in development for the treatment of patients with anaplastic lymphoma kinase positive (ALK ) non-small cell cancer (NSCLC) whose disease is resistant to crizotinib. Brigatinib is currently being evaluated in the global Phase 2 ALTA (ALK in Lung Cancer Trial of AP26113) trial that is anticipated to form the basis for its initial regulatory review. ARIAD has also initiated the Phase 3 ALTA 1L trial to assess the efficacy of brigatinib in comparison to crizotinib. Brigatinib was granted orphan drug designation by the U.S. Food and Drug Administration (FDA) in May 2016 for the treatment of certain subtypes of non-small cell lung cancer (NSCLC). The designation is for anaplastic lymphoma kinase-positive (ALK ), c-ros 1 oncogene positive (ROS1 ), or epidermal growth factor receptor positive (EGFR ) non-small cell lung cancer (NSCLC). Brigatinib received breakthrough therapy designation from the FDA in October 2014 for the treatment of patients with ALK NSCLC whose disease is resistant to crizotinib. Both designations were based on results from an ongoing Phase 1/2 trial that showed anti-tumor activity of brigatinib in patients with ALK NSCLC, including patients with active brain metastases.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4247 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21502504 |
0.62 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ALUNBRIG Approved UseALUNBRIG is indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung
cancer (NSCLC) who have progressed on or are intolerant to crizotinib. Launch Date2017 |
|||
| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
552 ng/mL |
180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BRIGATINIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
701.3 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
BRIGATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
8165 ng × h/mL |
180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BRIGATINIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13261 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
BRIGATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
25 h |
180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BRIGATINIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
31 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
BRIGATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
34% |
180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BRIGATINIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
Disc. AE: Pneumonitis, Pneumonitis... Other AEs: Nausea, Nausea... AEs leading to discontinuation/dose reduction: Pneumonitis (all grades, 37%) Other AEs:Pneumonitis (grade 3-4, 1.8%) Hypertension (grade 3-4, 5.5%) Pneumonia (all grades, 4.6%) Pneumonia (grade 3-4, 1.83%) Hyperglycemia (grade 3-4, 3.7%) Creatine phosphokinase increased (all grades, 27%) Creatine phosphokinase increased (grade 3-4, 2.8%) Nausea (all grades, 33%) Sources: Nausea (grade 3-4, 0.9%) Diarrhea (all grades, 19%) Vomiting (all grades, 24%) Vomiting (grade 3-4, 1.8%) Constipation (all grades, 19%) Constipation (grade 3-4, 0.9%) Abdominal distension (all grades, 17%) Abdominal pain (all grades, 17%) Epigastric discomfort (all grades, 17%) Asthenia (all grades, 29%) Asthenia (grade 3-4, 1.8%) Fatigue (all grades, 29%) Fatigue (grade 3-4, 1.8%) Pyrexia (all grades, 14%) Cough (all grades, 18%) Dyspnea (all grades, 27%) Dyspnea (grade 5, 1 patient) Exertional dyspnea (all grades, 27%) Dyspnea (grade 3-4, 2.8%) Exertional dyspnea (grade 3-4, 2.8%) Hypoxia (all grades, 0.9%) Headache (all grades, 28%) Sinus headache (all grades, 28%) Peripheral sensory neuropathy (all grades, 13%) Paresthesia (all grades, 13%) Peripheral sensory neuropathy (grade 3-4, 0.9%) Paresthesia (grade 3-4, 0.9%) Acneiform dermatitis (all grades, 15%) Exfoliative rash (all grades, 15%) Rash (all grades, 15%) Pruritic rash (all grades, 15%) Pustular rash (all grades, 15%) Acneiform dermatitis (grade 3-4, 1.8%) Exfoliative rash (grade 3-4, 1.8%) Rash (grade 3-4, 1.8%) Pruritic rash (grade 3-4, 1.8%) Pustular rash (grade 3-4, 1.8%) Hypertension (all grades, 11%) Muscle spasms (all grades, 12%) Back pain (all grades, 10%) Back pain (grade 3-4, 1.8%) Musculoskeletal pain (all grades, 9.2%) Myalgia (all grades, 9.2%) Arthralgia (all grades, 14%) Arthralgia (grade 3-4, 0.9%) Pain in extremity (all grades, 11%) Decreased appetite (all grades, 22%) Decreased appetite (grade 3-4, 0.9%) Diplopia (all grades, 7.3%) Photophobia (all grades, 7.3%) Blurred vision (all grades, 7.3%) Visual acuity reduced (all grades, 7.3%) Visual impairment (all grades, 7.3%) Vitreous floaters (all grades, 7.3%) Visual field defect (all grades, 7.3%) Macular edema (all grades, 7.3%) Vitreous detachment (all grades, 7.3%) Pneumonia (grade 5, 1 patient) Insomnia (all grades, 11%) Aspartate aminotransferase increased (all grades, 38%) Aspartate aminotransferase increased (grade 3-4, 0.9%) Hyperglycemia (all grades, 38%) Lipase increased (all grades, 21%) Lipase increased (grade 3-4, 4.6%) Alanine aminotransferase increased (all grades, 34%) Amylase increased (all grades, 27%) Amylase increased (grade 3-4, 3.7%) Alkaline phosphatase increased (all grades, 15%) Alkaline phosphatase increased (grade 3-4, 0.9%) Phosphate decreased (all grades, 15%) Phosphate decreased (grade 3-4, 1.8%) Anemia (all grades, 23%) Anemia (grade 3-4, 0.9%) Lymphopenia (all grades, 19%) Lymphopenia (grade 3-4, 2.8%) Respiratory failure (grade 5, 1 patient) Pulmonary embolism (grade 5, 1 patient) Bacterial meningitis (grade 5, 1 patient) Urosepsis (grade 5, 1 patient) |
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy |
DLT: Dyspnea, Hypoxia... Dose limiting toxicities: Dyspnea (1 patient) Sources: Hypoxia (1 patient) |
240 mg 1 times / day multiple, oral Dose: 240 mg, 1 times / day Route: oral Route: multiple Dose: 240 mg, 1 times / day Sources: |
unhealthy |
DLT: Alanine aminotransferase increased... Dose limiting toxicities: Alanine aminotransferase increased (1 patient) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Hypoxia | all grades, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Back pain | all grades, 10% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Hypertension | all grades, 11% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Insomnia | all grades, 11% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pain in extremity | all grades, 11% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Muscle spasms | all grades, 12% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Paresthesia | all grades, 13% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Peripheral sensory neuropathy | all grades, 13% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Arthralgia | all grades, 14% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pyrexia | all grades, 14% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Acneiform dermatitis | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Alkaline phosphatase increased | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Exfoliative rash | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Phosphate decreased | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pruritic rash | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pustular rash | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Rash | all grades, 15% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Abdominal distension | all grades, 17% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Abdominal pain | all grades, 17% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Epigastric discomfort | all grades, 17% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Cough | all grades, 18% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Constipation | all grades, 19% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Diarrhea | all grades, 19% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Lymphopenia | all grades, 19% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Lipase increased | all grades, 21% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Decreased appetite | all grades, 22% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Anemia | all grades, 23% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Vomiting | all grades, 24% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Amylase increased | all grades, 27% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Dyspnea | all grades, 27% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Exertional dyspnea | all grades, 27% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Creatine phosphokinase increased | all grades, 27% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Headache | all grades, 28% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Sinus headache | all grades, 28% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Asthenia | all grades, 29% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Fatigue | all grades, 29% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Nausea | all grades, 33% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Alanine aminotransferase increased | all grades, 34% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pneumonitis | all grades, 37% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Aspartate aminotransferase increased | all grades, 38% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Hyperglycemia | all grades, 38% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pneumonia | all grades, 4.6% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Blurred vision | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Diplopia | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Macular edema | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Photophobia | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Visual acuity reduced | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Visual field defect | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Visual impairment | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Vitreous detachment | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Vitreous floaters | all grades, 7.3% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Musculoskeletal pain | all grades, 9.2% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Myalgia | all grades, 9.2% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Alkaline phosphatase increased | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Anemia | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Arthralgia | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Aspartate aminotransferase increased | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Constipation | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Decreased appetite | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Nausea | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Paresthesia | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Peripheral sensory neuropathy | grade 3-4, 0.9% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Acneiform dermatitis | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Asthenia | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Back pain | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Exfoliative rash | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Fatigue | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Phosphate decreased | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pruritic rash | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pustular rash | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Rash | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Vomiting | grade 3-4, 1.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pneumonitis | grade 3-4, 1.8% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pneumonia | grade 3-4, 1.83% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Dyspnea | grade 3-4, 2.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Exertional dyspnea | grade 3-4, 2.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Lymphopenia | grade 3-4, 2.8% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Creatine phosphokinase increased | grade 3-4, 2.8% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Amylase increased | grade 3-4, 3.7% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Hyperglycemia | grade 3-4, 3.7% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Lipase increased | grade 3-4, 4.6% | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Hypertension | grade 3-4, 5.5% Disc. AE |
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Bacterial meningitis | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Dyspnea | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pneumonia | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Pulmonary embolism | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Respiratory failure | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Urosepsis | grade 5, 1 patient | 180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: |
unhealthy, 54 years (range: 18 - 82 years) Health Status: unhealthy Age Group: 54 years (range: 18 - 82 years) Sex: M+F Sources: |
| Dyspnea | 1 patient DLT, Disc. AE |
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy |
| Hypoxia | 1 patient DLT, Disc. AE |
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy |
| Alanine aminotransferase increased | 1 patient DLT |
240 mg 1 times / day multiple, oral Dose: 240 mg, 1 times / day Route: oral Route: multiple Dose: 240 mg, 1 times / day Sources: |
unhealthy |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| weak | unlikely Comment: Induction of CYP3A4 mRNA (mean 6-fold change at 1 μM), but no induction of CYP3A4 activity. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=43 Page: - |
|||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | yes (co-administration study) Comment: Coadministration of gemfibrozil (a strong CYP2C8 inhibitor) 600 mg BID with a single dose of 90 mg brigatinib decreased brigatinib AUC by 12% (90% CI: 6%, 17%) and Cmax by 41% (90% CI: 35%, 46%) as compared with brigatinib alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: - |
|||
| minor | yes (co-administration study) Comment: Coadministration of itraconazole (a strong CYP3A4 inhibitor) increased brigatinib AUC by 2-fold. Coadministration of rifampin (a strong CYP3A4 inducer) decreased brigatinib AUC by 80% (90% CI: 79%, 82%) and Cmax by 60% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: - |
|||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes | ||||
| yes |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02094573
90 mg tablet, taken orally once daily,continuously in a 28-day cycle
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27049722
Brigatinib inhibited ALK phosphorylation in a dose-dependent manner, and at 50 nM brigatinib, phosphorylation of ALK was abolished in ALK addicted neuroblastoma lines
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:39:37 GMT 2025
by
admin
on
Mon Mar 31 22:39:37 GMT 2025
|
| Record UNII |
HYW8DB273J
|
| Record Status |
Validated (UNII)
|
| Record Version |
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-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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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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Systematic Name | 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 | ||
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Brand Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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WHO-ATC |
L01XE43
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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NCI_THESAURUS |
C129825
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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FDA ORPHAN DRUG |
505415
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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NDF-RT |
N0000175605
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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NCI_THESAURUS |
C1967
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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CHEMBL3545311
Created by
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PRIMARY | |||
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1197953-54-0
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5233
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PRIMARY | |||
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Brigatinib
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HYW8DB273J
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admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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PRIMARY | |||
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C98831
Created by
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HYW8DB273J
Created by
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PRIMARY | |||
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DB12267
Created by
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100000170772
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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Brigatinib
Created by
admin on Mon Mar 31 22:39:37 GMT 2025 , Edited by admin on Mon Mar 31 22:39:37 GMT 2025
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DTXSID501027929
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1921217
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68165256
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10085
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SUB184911
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m12099
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BC-12
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TRANSPORTER -> SUBSTRATE | |||
|
TARGET -> INHIBITOR |
INHIBITOR
IC50
|
||
|
TRANSPORTER -> SUBSTRATE | |||
|
|
TARGET -> INHIBITOR | |||
|
|
TARGET -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
EXCRETED UNCHANGED |
FECAL
|
||
|
|
TARGET -> INHIBITOR |
IC50
|
||
|
EXCRETED UNCHANGED |
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
|
TARGET -> INHIBITOR |
IC50
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
IC50
|
||
|
|
TARGET -> INHIBITOR |
IC50
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
|
TARGET -> INHIBITOR |
IC50
|
||
|
|
TARGET -> INHIBITOR |
IC50
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
METABOLITE -> PARENT |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
|
|
|||
| Tmax | PHARMACOKINETIC |
|
|
|||
| Volume of Distribution | PHARMACOKINETIC |
|
|
|||
| Volume of Distribution |
|
|
||||