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Details

Stereochemistry ACHIRAL
Molecular Formula C29H39ClN7O2P
Molecular Weight 584.0935
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BRIGATINIB

SMILES

CN1CCN(CC1)C2CCN(CC2)c3ccc(c(c3)OC)Nc4ncc(c(=Nc5ccccc5P(=O)(C)C)[nH]4)Cl

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)

HIDE SMILES / InChI

Description
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ALUNBRIG

Approved Use

ALUNBRIG 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 Date

1.49325126E12
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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%)
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%)
Other AEs:
Nausea (all grades, 33%)
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)
Sources:
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)
Hypoxia (1 patient)
Sources:
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

AEs

AESignificanceDosePopulation
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical 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.
Page: -
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical 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.
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%
Page: -
no
no
no
no
no
no
no
no
no
yes
yes
Tox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice.
2016 May 17
Patents

Patents

Sample Use Guides

90 mg tablet, taken orally once daily,continuously in a 28-day cycle
Route of Administration: Oral
Brigatinib inhibited ALK phosphorylation in a dose-dependent manner, and at 50 nM brigatinib, phosphorylation of ALK was abolished in ALK addicted neuroblastoma lines
Name Type Language
BRIGATINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
BRIGATINIB [ORANGE BOOK]
Common Name English
BRIGATINIB [WHO-DD]
Common Name English
AP26113
Code English
5-CHLORO-N4-(2-(DIMETHYLPHOSPHORYL)PHENYL)-N2-(2-METHOXY-4-(4-(4-METHYLPIPERAZIN-1- YL)PIPERIDIN-1-YL)PHENYL)PYRIMIDINE-2,4-DIAMINE
Systematic Name English
BRIGATINIB [USAN]
Common Name English
(2-((5-CHLORO-2-((2-METHOXY-4-(4-(4-METHYLPIPERAZIN-1-YL)PIPERIDIN-1-YL)PHENYL)AMINO)PYRIMIDIN-4-YL)AMINO)PHENYL)DIMETHYL-,.DELTA.5-PHOSPHANONE
Systematic Name English
2,4-PYRIMIDINEDIAMINE, 5-CHLORO-N4-(2-(DIMETHYLPHOSPHINYL)PHENYL)-N2-(2-METHOXY-4-(4-(4-METHYL-1-PIPERAZINYL)-1-PIPERIDINYL)PHENYL)-
Systematic Name English
ALUNBRIG
Brand Name English
AP-26113
Code English
BRIGATINIB [MI]
Common Name English
BRIGATINIB [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC L01XE43
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
FDA ORPHAN DRUG 505415
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL3545311
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
CAS
1197953-54-0
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
DRUG CENTRAL
5233
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
LACTMED
Brigatinib
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
NCI_THESAURUS
C98831
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
FDA UNII
HYW8DB273J
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
DRUG BANK
DB12267
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
WIKIPEDIA
Brigatinib
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
RXCUI
1921217
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
PUBCHEM
68165256
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
INN
10085
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
EVMPD
SUB184911
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY
MERCK INDEX
M12099
Created by admin on Sat Jun 26 16:27:31 UTC 2021 , Edited by admin on Sat Jun 26 16:27:31 UTC 2021
PRIMARY