U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C28H36ClN5O3S
Molecular Weight 558.135
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CERITINIB

SMILES

CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(=O)C(C)C)=N3

InChI

InChIKey=VERWOWGGCGHDQE-UHFFFAOYSA-N
InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34)

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=2467504; https://www.novartis.ca/sites/www.novartis.ca/files/zykadia_scrip_e.pdf

Ceritinib is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). Ceritinib is approved by FDA and is indicated for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer. Ceritinib also targets insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1.

CNS Activity

CNS Penetrant
2554
Curator's Comment: Ceritinib crossed the blood-brain barrier in rats with a brain-to-blood exposure ratio of approximately 15%

Originator

Approval Year

2014
494
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 0.15 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
ZYKADIA

Approved Use

ZYKADIA 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

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
800 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28740365
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
16500 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28740365
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
40 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28740365
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
3%
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28740365
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CERITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (all grades, 100%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (all grades, 33%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Other AEs: Vomiting, Abdominal pain...
Other AEs:
Vomiting (all grades, 100%)
Abdominal pain (all grades, 17%)
Fatigue (all grades, 33%)
Blood creatinine increased (all grades, 50%)
Decreased appetite (all grades, 50%)
Alanine aminotransferase increased (all grades, 33%)
Aspartate aminotransferase increased (all grades, 33%)
Neutropenia (all grades, 33%)
Rash (all grades, 50%)
Maculopapular rash (17%)
Stomatitis (33%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125/
unhealthy, 39 years (range: 34–61 years)
n = 4
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 39 years (range: 34–61 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125/
DLT: Lipase increased...
Dose limiting toxicities:
Lipase increased (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125/
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Disc. AE: Pneumonitis...
Other AEs: Pneumonitis...
AEs leading to
discontinuation/dose reduction:
Pneumonitis (grade 3-4, 3%)
Other AEs:
Pneumonitis (all grades, 4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
DLT: ALT increased, AST increased...
Disc. AE: Nausea, Diarrhea...
Other AEs: Nausea, Diarrhea...
Dose limiting toxicities:
ALT increased (grade 3-4, 34%)
AST increased (grade 3-4, 21%)
AEs leading to
discontinuation/dose reduction:
Nausea (grade 3-4, 2.6%)
Diarrhea (grade 3-4, 4.8%)
Vomiting (grade 3-4, 5%)
GGT increased (grade 3-4, 49%)
Creatinine increased (grade 3-4, 4.2%)
Amylase increased (grade 3-4, 8%)
Lipase increased (grade 3-4, 6%)
Other AEs:
Nausea (all grades, 69%)
Diarrhea (all grades, 85%)
Vomiting (all grades, 67%)
Abdominal pain (all grades, 40%)
Abdominal pain upper (all grades, 40%)
Abdominal discomfort (all grades, 40%)
Epigastric discomfort (all grades, 40%)
Abdominal pain (grade 3-4, 3.7%)
Abdominal pain upper (grade 3-4, 3.7%)
Abdominal discomfort (grade 3-4, 3.7%)
Epigastric discomfort (grade 3-4, 3.7%)
Constipation (all grades, 20%)
Dyspepsia (all grades, 15%)
Gastroesophageal reflux disease (all grades, 15%)
Dysphagia (all grades, 15%)
Dyspepsia (grade 3-4, 0.5%)
Gastroesophageal reflux disease (grade 3-4, 0.5%)
Dysphagia (grade 3-4, 0.5%)
Fatigue (all grades, 45%)
Asthenia (all grades, 45%)
Fatigue (grade 3-4, 7%)
Asthenia (grade 3-4, 7%)
Non-cardiac chest pain (all grades, 21%)
Non-cardiac chest pain (grade 3-4, 1.1%)
Back pain (all grades, 19%)
Back pain (grade 3-4, 1.6%)
Pyrexia (all grades, 19%)
Pain in extremity (all grades, 13%)
Musculoskeletal pain (all grades, 11%)
Musculoskeletal pain (grade 3-4, 0.5%)
Pruritus (all grades, 11%)
Pruritus (grade 3-4, 0.5%)
Decreased appetite (all grades, 34%)
Decreased appetite (grade 3-4, 1.1%)
Weight loss (all grades, 24%)
Weight loss (grade 3-4, 3.7%)
Rash (all grades, 21%)
Dermatitis acneiform (all grades, 21%)
Rash maculo-papular (all grades, 21%)
Rash (grade 3-4, 1.1%)
Dermatitis acneiform (grade 3-4, 1.1%)
Rash maculo-papular (grade 3-4, 1.1%)
Headache (all grades, 19%)
Headache (all grades, 0.5%)
Dizziness (grade 3-4, 12%)
Dizziness (grade 3-4, 1.1%)
QT interval prolonged (all grades, 12%)
QT interval prolonged (grade 3-4, 2.6%)
Pericardial effusion (all grades, 4.2%)
Pericarditis (all grades, 4.2%)
Pericardial effusion (grade 3-4, 1.6%)
Pericarditis (grade 3-4, 1.6%)
Cough (all grades, 25%)
Pneumonia (serious, 4%)
Pleural effusion (serious, 4%)
ALT increased (all grades, 91%)
AST increased (all grades, 86%)
GGT increased (all grades, 84%)
Alkaline phosphatase increased (all grades, 81%)
Alkaline phosphatase increased (grade 3-4, 12%)
Creatinine increased (all grades, 77%)
Hyperglycemia (all grades, 53%)
Hyperglycemia (grade 3-4, 10%)
Hypophosphatemia (all grades, 38%)
Hypophosphatemia (grade 3-4, 3.7%)
Amylase increased (all grades, 37%)
Hyperbilirubinemia (all grades, 15%)
Hyperbilirubinemia (grade 3-4, 0.5%)
Lipase increased (all grades, 13%)
Anemia (all grades, 67%)
Anemia (grade 3-4, 4.2%)
Neutropenia (all grades, 27%)
Neutropenia (grade 3-4, 2.1%)
Thrombocytopenia (all grades, 16%)
Thrombocytopenia (grade 3-4, 1%)
Vision decreased (4%)
Blurred vision (4%)
Photopsia (4%)
Accommodation disorder (4%)
Presbyopia (4%)
Visual acuity reduced (4%)
Vitreous floaters (4%)
Bradycardia (4%)
Hepatotoxicity (2%)
Renal failure (2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Nausea all grades, 100%
Disc. AE
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Diarrhea all grades, 33%
Disc. AE
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Maculopapular rash 17%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Stomatitis 33%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Vomiting all grades, 100%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Abdominal pain all grades, 17%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Alanine aminotransferase increased all grades, 33%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Aspartate aminotransferase increased all grades, 33%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Fatigue all grades, 33%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Neutropenia all grades, 33%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Blood creatinine increased all grades, 50%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Decreased appetite all grades, 50%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Rash all grades, 50%
450 mg 1 times / day steady, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: steady
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
unhealthy, 37 years (range: 29–67 years)
n = 6
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 37 years (range: 29–67 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
Lipase increased grade 3, 1 patient
DLT, Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125/
unhealthy, 39 years (range: 34–61 years)
n = 4
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 39 years (range: 34–61 years)
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125/
Pneumonitis all grades, 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pneumonitis grade 3-4, 3%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hepatotoxicity 2%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Renal failure 2%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Accommodation disorder 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Blurred vision 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Bradycardia 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Photopsia 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Presbyopia 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Vision decreased 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Visual acuity reduced 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Vitreous floaters 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Headache all grades, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Musculoskeletal pain all grades, 11%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pruritus all grades, 11%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
QT interval prolonged all grades, 12%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Lipase increased all grades, 13%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pain in extremity all grades, 13%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dyspepsia all grades, 15%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dysphagia all grades, 15%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Gastroesophageal reflux disease all grades, 15%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hyperbilirubinemia all grades, 15%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Thrombocytopenia all grades, 16%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Back pain all grades, 19%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Headache all grades, 19%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pyrexia all grades, 19%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Constipation all grades, 20%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dermatitis acneiform all grades, 21%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Non-cardiac chest pain all grades, 21%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Rash maculo-papular all grades, 21%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Rash all grades, 21%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Weight loss all grades, 24%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Cough all grades, 25%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Neutropenia all grades, 27%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Decreased appetite all grades, 34%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Amylase increased all grades, 37%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hypophosphatemia all grades, 38%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pericardial effusion all grades, 4.2%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pericarditis all grades, 4.2%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal discomfort all grades, 40%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal pain upper all grades, 40%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal pain all grades, 40%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Epigastric discomfort all grades, 40%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Asthenia all grades, 45%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Fatigue all grades, 45%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hyperglycemia all grades, 53%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Anemia all grades, 67%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Vomiting all grades, 67%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Nausea all grades, 69%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Creatinine increased all grades, 77%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Alkaline phosphatase increased all grades, 81%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
GGT increased all grades, 84%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Diarrhea all grades, 85%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
AST increased all grades, 86%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
ALT increased all grades, 91%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dyspepsia grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dysphagia grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Gastroesophageal reflux disease grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hyperbilirubinemia grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Musculoskeletal pain grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pruritus grade 3-4, 0.5%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Thrombocytopenia grade 3-4, 1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Decreased appetite grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dermatitis acneiform grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dizziness grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Non-cardiac chest pain grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Rash maculo-papular grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Rash grade 3-4, 1.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Back pain grade 3-4, 1.6%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pericardial effusion grade 3-4, 1.6%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pericarditis grade 3-4, 1.6%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hyperglycemia grade 3-4, 10%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Alkaline phosphatase increased grade 3-4, 12%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Dizziness grade 3-4, 12%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Neutropenia grade 3-4, 2.1%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
QT interval prolonged grade 3-4, 2.6%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Nausea grade 3-4, 2.6%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
AST increased grade 3-4, 21%
DLT, Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal discomfort grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal pain upper grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Abdominal pain grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Epigastric discomfort grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Hypophosphatemia grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Weight loss grade 3-4, 3.7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
ALT increased grade 3-4, 34%
DLT, Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Anemia grade 3-4, 4.2%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Creatinine increased grade 3-4, 4.2%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Diarrhea grade 3-4, 4.8%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
GGT increased grade 3-4, 49%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Vomiting grade 3-4, 5%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Lipase increased grade 3-4, 6%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Asthenia grade 3-4, 7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Fatigue grade 3-4, 7%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Amylase increased grade 3-4, 8%
Disc. AE
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pleural effusion serious, 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Pneumonia serious, 4%
750 mg 1 times / day steady, oral
MTD
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
unhealthy, 54 years (range: 22- 81 years)
n = 189
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 54 years (range: 22- 81 years)
Sex: M+F
Population Size: 189
Sources:
https://pubmed.ncbi.nlm.nih.gov/26020125
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587

inducer
781
inhibitor
1767

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2A6
707

CYP2B6
810

CYP2C19
1478

CYP2E1
882

P-gp
1461

BCRP
699

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

OCT2
647

OCT1
512
CYP3A
191

P-gp
1537

BCRP
561

OCT1
327

OAT2
115

OATP1B1
406

OATP2B1
104
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
773
 no
OAT3
644
 no
OCT1
543
 no
P-gp
1650
 no
CYP3A4
1925
 yes [IC50 0.2 uM]
CYP2B6
1001
 yes [IC50 2 uM]
CYP2C9
1819
 yes [IC50 2 uM]
CYP2D6
1891
 yes [IC50 20 uM]
CYP2E1
970
 yes [IC50 30 uM]
CYP2A6
739
 yes [IC50 5 uM]
CYP2C19
1553
 yes [IC50 70 uM]
OAT1
603
 yes [Inhibition 5 uM]
OATP1B1
803
 yes [Inhibition 5 uM]
OATP1B3
715
 yes [Inhibition 5 uM]
OCT2
648
 yes [Inhibition 5 uM]
CYP1A2
1692
 yes
CYP2B6
1001
 yes
CYP2C9
1819
 yes
CYP3A4
1925
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A
191
 major
yes (co-administration study)
Comment: Ceritinib is primarily metabolized by CYP3A, and is also a reversible and time-dependent inhibitor of CYP3A in vitro. Coadministration of ketoconazole (a strong CYP3A inhibitor) 200 mg twice daily for 14 days and a single dose of 450 mg ceritinib increased ceritinib AUC by 2.9- fold and Cmax by 20% in healthy subjects. Coadministration of rifampin (a strong CYP3A inducer) 600 mg daily for 14 days and a single dose of 750 mg ceritinib decreased ceritinib AUC by 70% and Cmax by 44% in healthy subjects.
Page: -
OAT2
115
 no
OATP1B1
406
 no
OATP2B1
104
 no
OCT1
327
 no
P-gp
1537
 yes
BCRP
561
 yes
no (co-administration study)
Comment: Ko143 (a BCRP inhibitor) had a smaller effect on the reduction of efflux ratio to 121 at 3 μM ceritinib, indicating that an in vivo DDI study with a BCRP inhibitor is not necessary.
Page: -
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:78432
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:78432
ChemicalBook
CB82652832
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB82652832
MolPort
MolPort-035-395-774
https://www.molport.com/shop/molecule-link/MolPort-035-395-774
Selleck Chemicals
ldk378
http://www.selleckchem.com/products/ldk378.html
ZINC
ZINC000096272772
http://zinc15.docking.org/substances/ZINC000096272772
PubMed

PubMed

TitleDatePubMed
Phase I Study of Ceritinib (LDK378) in Japanese Patients with Advanced, Anaplastic Lymphoma Kinase-Rearranged Non-Small-Cell Lung Cancer or Other Tumors.
2015 Jul
Patents

Patents

08039479
29
08372858
30
08377921
29
08399450
29

Sample Use Guides

In Vivo Use Guide
750 mg orally once daily. Administer ZYKADIA on an empty stomach (i.e., do not administer within 2 hours of a meal).
Route of Administration: Oral
In Vitro Use Guide
In vitro Ceritinib inhibited ALK+-NSCLC cell lines (H3112 and H2228) with GIC50 values of 6.3 and 3.8 nM.
Name Type Language
CERITINIB
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CERITINIB [MI]
Common Name English
2,4-PYRIMIDINEDIAMINE, 5-CHLORO-N4-(2-((1-METHYLETHYL)SULFONYL)PHENYL)-N2-(5-METHYL-2-(1-METHYLETHOXY)-4-(4-PIPERIDINYL)PHENYL)-
Systematic Name English
CERITINIB [ORANGE BOOK]
Common Name English
CERITINIB [USAN]
Common Name English
ceritinib [INN]
Common Name English
NVP-LDK-378-NX
Code English
LDK-378
Code English
5-CHLORO-N4-(2-((1-METHYLETHYL)SULFONYL)PHENYL)-N2-(5-METHYL-2-(1-METHYLETHOXY)-4- (PIPERIDIN-4-YL)PHENYL)PYRIMIDINE-2,4-DIAMINE
Systematic Name English
ZYKADIA
Brand Name English
LDK378
Code English
5-CHLORO-N2-(5-METHYL-4-(PIPERIDIN-4-YL)-2-(PROPAN-2-YLOXY)PHENYL)-N4-(2-(PROPANE-2- SULFONYL)PHENYL)PYRIMIDINE-2,4-DIAMINE
Systematic Name English
NVP-LDK378-NX
Code English
CERITINIB [JAN]
Common Name English
CERITINIB [VANDF]
Common Name English
Ceritinib [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C141136
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
WHO-ATC L01XE28
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
FDA ORPHAN DRUG 405213
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
NDF-RT N0000175605
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
Code System Code Type Description
INN
9817
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
EU-Orphan Drug
5-chloro-N2-[2-isopropoxy(-5-methyl-4-...(NEGATIVE)
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY Treatment of non-small cell lung cancer (NSCLC) that is anaplastic lymphoma kinase (ALK)-positive 28/03/2014 Negative
LACTMED
Ceritinib
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
NDF-RT
N0000185504
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
NDF-RT
N0000020000
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
NDF-RT
N0000190114
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
DAILYMED
K418KG2GET
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
MERCK INDEX
m11724
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
CAS
1032900-25-6
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
CHEBI
78432
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
NCI_THESAURUS
C115112
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
USAN
BC-20
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
EVMPD
SUB130802
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
SMS_ID
100000156788
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
WIKIPEDIA
Ceritinib
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
IUPHAR
7397
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
DRUG BANK
DB09063
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
ChEMBL
CHEMBL2403108
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
RXCUI
1535457
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY RxNorm
DRUG CENTRAL
4866
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
EPA CompTox
DTXSID10725373
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
PUBCHEM
57379345
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
PRIMARY
FDA UNII
K418KG2GET
Created by admin on Sat Dec 16 09:50:00 GMT 2023 , Edited by admin on Sat Dec 16 09:50:00 GMT 2023
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ACTIVE MOIETY
Structure of CERITINIB
NIH
NCATS
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