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
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)
DescriptionCurator'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
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
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12150792
Curator's Comment: Ceritinib crossed the blood-brain barrier in rats with a brain-to-blood exposure ratio of approximately 15%
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4247 |
0.15 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ZYKADIA Approved UseZYKADIA 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 Date2014 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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%) Sources: 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%) |
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%) AEs leading toAST increased (grade 3-4, 21%) discontinuation/dose reduction: Nausea (grade 3-4, 2.6%) Other AEs: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%) Nausea (all grades, 69%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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
Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205755Orig1s000ClinPharmR.pdf#page=20 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205755Orig1s000ClinPharmR.pdf#page=49 Page: - |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. | 2007 Jan 2 |
|
The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. | 2014 Jun |
|
Overcoming drug resistance in ALK-rearranged lung cancer. | 2014 Mar 27 |
|
The EML4-ALK oncogene: targeting an essential growth driver in human cancer. | 2015 |
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 Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=24675041
In vitro Ceritinib inhibited ALK+-NSCLC cell lines (H3112 and H2228) with GIC50 values of 6.3 and 3.8 nM.
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Classification Tree | Code System | Code | ||
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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
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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
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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
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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
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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
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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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
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PRIMARY | |||
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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
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PRIMARY | Treatment of non-small cell lung cancer (NSCLC) that is anaplastic lymphoma kinase (ALK)-positive 28/03/2014 Negative | ||
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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
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PRIMARY | |||
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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
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PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] | ||
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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
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PRIMARY | Receptor Tyrosine Kinase Inhibitors [MoA] | ||
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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
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PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
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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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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | RxNorm | ||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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
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PRIMARY | |||
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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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PRIMARY |
ACTIVE MOIETY