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Details

Stereochemistry ACHIRAL
Molecular Formula C28H36ClN5O3S
Molecular Weight 558.1372
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CERITINIB

SMILES

CC(C)Oc1cc(c(C)cc1Nc2ncc(c(=Nc3ccccc3S(=O)(=O)C(C)C)[nH]2)Cl)C4CCNCC4

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

Molecular Formula C28H36ClN5O3S
Molecular Weight 558.1372
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.15 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1.39872961E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
800 ng/mL
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
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
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%
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:
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:
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (all grades, 100%)
Sources:
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:
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:
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (all grades, 33%)
Sources:
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:
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:
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:
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
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:
DLT: Lipase increased...
Dose limiting toxicities:
Lipase increased (grade 3, 1 patient)
Sources:
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:
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
Disc. AE: Pneumonitis...
Other AEs: Pneumonitis...
AEs leading to
discontinuation/dose reduction:
Pneumonitis (grade 3-4, 3%)
Other AEs:
Pneumonitis (all grades, 4%)
Sources:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
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:
unhealthy, 53 years
n = 255
Health Status: unhealthy
Condition: ALK-positive NSCLC patients
Age Group: 53 years
Sex: M+F
Population Size: 255
Sources:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
yes [IC50 0.2 uM]
yes [IC50 2 uM]
yes [IC50 2 uM]
yes [IC50 20 uM]
yes [IC50 30 uM]
yes [IC50 5 uM]
yes [IC50 70 uM]
yes [Inhibition 5 uM]
yes [Inhibition 5 uM]
yes [Inhibition 5 uM]
yes [Inhibition 5 uM]
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
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: -
no
no
no
no
yes
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

PubMed

PubMed

TitleDatePubMed
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
2007 Jan 2
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
2013 Jul 25
Overcoming drug resistance in ALK-rearranged lung cancer.
2014 Mar 27
The EML4-ALK oncogene: targeting an essential growth driver in human cancer.
2015
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

Sample Use Guides

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 Ceritinib inhibited ALK+-NSCLC cell lines (H3112 and H2228) with GIC50 values of 6.3 and 3.8 nM.
Substance Class Chemical
Created
by admin
on Sat Jun 26 01:47:55 UTC 2021
Edited
by admin
on Sat Jun 26 01:47:55 UTC 2021
Record UNII
K418KG2GET
Record Status Validated (UNII)
Record Version
  • Download
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 [WHO-DD]
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
Classification Tree Code System Code
NCI_THESAURUS C141136
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
WHO-ATC L01XE28
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
FDA ORPHAN DRUG 405213
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
Code System Code Type Description
INN
9817
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
EU-Orphan Drug
5-chloro-N2-[2-isopropoxy(-5-methyl-4-...(NEGATIVE)
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
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 Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
NDF-RT
N0000185504
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
NDF-RT
N0000020000
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
NDF-RT
N0000190114
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
MERCK INDEX
M11724
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
CAS
1032900-25-6
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
NCI_THESAURUS
C115112
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
EVMPD
SUB130802
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
WIKIPEDIA
Ceritinib
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
IUPHAR
7397
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
DRUG BANK
DB09063
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
ChEMBL
CHEMBL2403108
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
RXCUI
1535457
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4866
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
EPA CompTox
1032900-25-6
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
PUBCHEM
57379345
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
FDA UNII
K418KG2GET
Created by admin on Sat Jun 26 01:47:55 UTC 2021 , Edited by admin on Sat Jun 26 01:47:55 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> INHIBITOR
Midazolam is the substrate.
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> INHIBITOR
ceritinib also inhibits CYP2C9 in vitro.
METABOLIC ENZYME -> SUBSTRATE
RESPONSIBLE FOR 90 PERCENT OF METABOLISM
MAJOR
EXCRETED UNCHANGED
FECAL
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
INHIBITOR
IC50
Related Record Type Details
METABOLITE -> PARENT
IN-VIVO
FECAL
METABOLITE -> PARENT
IN-VIVO
FECAL; PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC