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=C(C=CC=C3)P(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)
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 |
10.0 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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 Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: |
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 Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: |
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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 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 Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: |
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 Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: |
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 Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: |
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
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Classification Tree | Code System | Code | ||
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WHO-ATC |
L01XE43
Created by
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NCI_THESAURUS |
C129825
Created by
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FDA ORPHAN DRUG |
505415
Created by
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NDF-RT |
N0000175605
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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NCI_THESAURUS |
C1967
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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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
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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PRIMARY | |||
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5233
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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PRIMARY | |||
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Brigatinib
Created by
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HYW8DB273J
Created by
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PRIMARY | |||
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C98831
Created by
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PRIMARY | |||
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HYW8DB273J
Created by
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DB12267
Created by
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PRIMARY | |||
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100000170772
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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PRIMARY | |||
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Brigatinib
Created by
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DTXSID501027929
Created by
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1921217
Created by
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PRIMARY | |||
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68165256
Created by
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PRIMARY | |||
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10085
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PRIMARY | |||
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SUB184911
Created by
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PRIMARY | |||
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m12099
Created by
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PRIMARY | |||
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BC-12
Created by
admin on Sat Dec 16 09:25:21 GMT 2023 , Edited by admin on Sat Dec 16 09:25:21 GMT 2023
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PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)