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Details

Stereochemistry ACHIRAL
Molecular Formula C30H34N4O2
Molecular Weight 482.6177
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ALECTINIB

SMILES

CCc1cc2c(cc1N3CCC(CC3)N4CCOCC4)C(C)(C)c5c(c6ccc(cc6[nH]5)C#N)C2=O

InChI

InChIKey=KDGFLJKFZUIJMX-UHFFFAOYSA-N
InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3

HIDE SMILES / InChI

Description
Curator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208434s000lbl.pdf

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group. Alectinib is specifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability. Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance. Alectinib is marketed as Alecensa.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.9 nM [IC50]
Target ID: SNU-2535
33.1 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Alecensa

Approved Use

ALECENSA is a kinase inhibitor 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

1.4497056E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
181 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ALECTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
665 ng/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALECTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
255 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
861 ng/mL
600 mg 2 times / day steady, oral
dose: 600 mg
route of administration: oral
experiment type: steady
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
107 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
85.5 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
306 ng/mL
600 mg 2 times / day steady, oral
dose: 600 mg
route of administration: oral
experiment type: steady
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
71.4 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
17.5 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
19.3 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2790 ng × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ALECTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
7430 ng × h/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALECTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1590 ng*h/mL
600 mg single, oral
dose: 600 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
7760 ng*h/mL
600 mg 2 times / day steady, oral
dose: 600 mg
route of administration: oral
experiment type: steady
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2820 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
3710 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2920 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
3850 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2890 ng*h/mL
600 mg 2 times / day steady, oral
dose: 600 mg
route of administration: oral
experiment type: steady
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
471 ng*h/mL
600 mg single, oral
dose: 600 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
465 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
583 ng*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
32 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ALECTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
33 h
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALECTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26.1 h
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
39.3 h
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
30.5 h
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
24.5 h
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
ALECTINIB METABOLITE M4 plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ALECTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 53 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 53 years
Sex: M+F
Population Size: 253
Sources:
Other AEs: Cough...
900 mg 2 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 2 times / day
Route: oral
Route: multiple
Dose: 900 mg, 2 times / day
Sources:
unhealthy, 56 years (range: 40–83 years)
n = 6
Health Status: unhealthy
Condition: locally advanced, or metastatic NSCLC
Age Group: 56 years (range: 40–83 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 3)
Sources:
900 mg 2 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 2 times / day
Route: oral
Route: multiple
Dose: 900 mg, 2 times / day
Sources:
unhealthy, 56 years (range: 40–83 years)
n = 6
Health Status: unhealthy
Condition: locally advanced, or metastatic NSCLC
Age Group: 56 years (range: 40–83 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Headache...
Dose limiting toxicities:
Headache (grade 3)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 134
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 134
Sources:
Other AEs: Hyperglycemia, Hyperglycemia...
Other AEs:
Hyperglycemia (all grades, 22%)
Hyperglycemia (grade 3-4, 2.2%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 143
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 143
Sources:
Other AEs: CPK increased, CPK increased...
Other AEs:
CPK increased (all grades, 37%)
CPK increased (grade 3-4, 2.8%)
Gamma-glutamyltransferase increased (all grades, 7%)
Gamma-glutamyltransferase increased (grade 3-4, 0.7%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 146
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 146
Sources:
Other AEs: Hypoalbuminemia...
Other AEs:
Hypoalbuminemia (all grades, 14%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Disc. AE: AST increased, ALT increased...
Other AEs: AST increased, Alkaline phosphatase increased...
AEs leading to
discontinuation/dose reduction:
AST increased (grade 3-4, 6%)
ALT increased (grade 3-4, 6%)
Other AEs:
AST increased (all grades, 50%)
Alkaline phosphatase increased (all grades, 50%)
ALT increased (all grades, 40%)
Creatinine increased (all grades, 38%)
Creatinine increased (grade 3-4, 4.1%)
Hypocalcemia (all grades, 29%)
Hyponatremia (all grades, 18%)
Hyponatremia (grade 3-4, 6%)
Hypokalemia (all grades, 17%)
Hypokalemia (grade 3-4, 2%)
Anemia (all grades, 62%)
Anemia (grade 3-4, 7%)
Lymphopenia (all grades, 14%)
Lymphopenia (grade 3-4, 1.4%)
Neutropenia (all grades, 14%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Disc. AE: Creatinine renal clearance decreased, Glomerular filtration rate decreased...
Other AEs: Glomerular filtration rate decreased, Acute kidney injury...
AEs leading to
discontinuation/dose reduction:
Creatinine renal clearance decreased (grade 3-4, 3.9%)
Glomerular filtration rate decreased (grade 3-4, 3.9%)
Acute kidney injury (grade 3-4, 3.9%)
Pneumonia (3.3%)
Hyperbilirubinemia (grade 3-4, 5%)
Other AEs:
Glomerular filtration rate decreased (all grades, 12%)
Acute kidney injury (all grades, 12%)
Constipation (all grades, 34%)
Nausea (all grades, 14%)
Nausea (grade 3-4, 0.7%)
Diarrhea (all grades, 12%)
Vomiting (all grades, 7%)
Fatigue (all grades, 26%)
Asthenia (all grades, 26%)
Fatigue (grade 3-4, 1.3%)
Asthenia (grade 3-4, 1.3%)
Peripheral edema (all grades, 22%)
Edema (all grades, 22%)
Eyelid edema (all grades, 22%)
Localized edema (all grades, 22%)
Face edema (all grades, 22%)
Peripheral edema (grade 3-4, 0.7%)
Edema (grade 3-4, 0.7%)
Eyelid edema (grade 3-4, 0.7%)
Localized edema (grade 3-4, 0.7%)
Face edema (grade 3-4, 0.7%)
Myalgia (all grades, 23%)
Musculoskeletal pain (all grades, 23%)
Rash (all grades, 15%)
Rash maculo-papular (all grades, 15%)
Dermatitis acneiform (all grades, 15%)
Erythema (all grades, 15%)
Generalized rash (all grades, 15%)
Rash macular (all grades, 15%)
Rash papular (all grades, 15%)
Exfoliative rash (all grades, 15%)
Pruritic rash (all grades, 15%)
Rash (grade 3-4, 0.7%)
Rash maculo-papular (grade 3-4, 0.7%)
Dermatitis acneiform (grade 3-4, 0.7%)
Erythema (grade 3-4, 0.7%)
Generalized rash (grade 3-4, 0.7%)
Rash macular (grade 3-4, 0.7%)
Rash papular (grade 3-4, 0.7%)
Exfoliative rash (grade 3-4, 0.7%)
Pruritic rash (grade 3-4, 0.7%)
Dysgeusia (all grades, 3.3%)
Hypogeusia (all grades, 3.3%)
Dysgeusia (grade 3-4, 0.7%)
Hypogeusia (grade 3-4, 0.7%)
Blurred vision (all grades, 4.6%)
Visual impairment (all grades, 4.6%)
Vitreous floaters (all grades, 4.6%)
Visual acuity reduced (all grades, 4.6%)
Diplopia (all grades, 4.6%)
Bradycardia (all grades, 11%)
Sinus bradycardia (all grades, 11%)
Blood creatinine increased (all grades, 12%)
Creatinine renal clearance decreased (all grades, 12%)
Blood creatinine increased (grade 3-4, 3.9%)
Cardiac arrest (grade 5, 1 patient)
Pneumonia (grade 5, 1 patient)
Hyperbilirubinemia (all grades, 54%)
Hyperkalemia (all grades, 12%)
Hyperkalemia (grade 3-4, 1.4%)
Hypophosphatemia (all grades, 9%)
Hypophosphatemia (grade 3-4, 1.4%)
Weight gain (9.9%)
Photosensitivity reaction (5.3%)
Stomatitis (3.3%)
Interstitial lung disease (1.3%)
Drug-induced liver injury (1.3%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Other AEs: Headache, Headache...
Other AEs:
Headache (all grades, 17%)
Headache (grade 3-4, 0.8%)
Dyspnea (all grades, 16%)
Dyspnea (grade 3-4, 3.17%)
Dyspnea (grade 5, 1 patient)
Back pain (all grades, 12%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Cough all grades, 19%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 53 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 53 years
Sex: M+F
Population Size: 253
Sources:
Neutropenia grade 3
DLT, Disc. AE
900 mg 2 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 2 times / day
Route: oral
Route: multiple
Dose: 900 mg, 2 times / day
Sources:
unhealthy, 56 years (range: 40–83 years)
n = 6
Health Status: unhealthy
Condition: locally advanced, or metastatic NSCLC
Age Group: 56 years (range: 40–83 years)
Sex: M+F
Population Size: 6
Sources:
Headache grade 3
DLT, Disc. AE
900 mg 2 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 2 times / day
Route: oral
Route: multiple
Dose: 900 mg, 2 times / day
Sources:
unhealthy, 56 years (range: 40–83 years)
n = 6
Health Status: unhealthy
Condition: locally advanced, or metastatic NSCLC
Age Group: 56 years (range: 40–83 years)
Sex: M+F
Population Size: 6
Sources:
Hyperglycemia all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 134
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 134
Sources:
Hyperglycemia grade 3-4, 2.2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 134
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 134
Sources:
CPK increased all grades, 37%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 143
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 143
Sources:
Gamma-glutamyltransferase increased all grades, 7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 143
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 143
Sources:
Gamma-glutamyltransferase increased grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 143
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 143
Sources:
CPK increased grade 3-4, 2.8%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 143
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 143
Sources:
Hypoalbuminemia all grades, 14%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 146
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 146
Sources:
Lymphopenia all grades, 14%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Neutropenia all grades, 14%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Hypokalemia all grades, 17%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Hyponatremia all grades, 18%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Hypocalcemia all grades, 29%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Creatinine increased all grades, 38%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
ALT increased all grades, 40%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
AST increased all grades, 50%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Alkaline phosphatase increased all grades, 50%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Anemia all grades, 62%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Lymphopenia grade 3-4, 1.4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Hypokalemia grade 3-4, 2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Creatinine increased grade 3-4, 4.1%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Hyponatremia grade 3-4, 6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
ALT increased grade 3-4, 6%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
AST increased grade 3-4, 6%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Anemia grade 3-4, 7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 147
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 147
Sources:
Drug-induced liver injury 1.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Interstitial lung disease 1.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Stomatitis 3.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Pneumonia 3.3%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Photosensitivity reaction 5.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Weight gain 9.9%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Bradycardia all grades, 11%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Sinus bradycardia all grades, 11%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Acute kidney injury all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Blood creatinine increased all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Creatinine renal clearance decreased all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Diarrhea all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Glomerular filtration rate decreased all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hyperkalemia all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Nausea all grades, 14%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Dermatitis acneiform all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Erythema all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Exfoliative rash all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Generalized rash all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Pruritic rash all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash macular all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash maculo-papular all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash papular all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash all grades, 15%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Edema all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Eyelid edema all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Face edema all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Localized edema all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Peripheral edema all grades, 22%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Musculoskeletal pain all grades, 23%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Myalgia all grades, 23%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Asthenia all grades, 26%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Fatigue all grades, 26%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Dysgeusia all grades, 3.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hypogeusia all grades, 3.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Constipation all grades, 34%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Blurred vision all grades, 4.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Diplopia all grades, 4.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Visual acuity reduced all grades, 4.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Visual impairment all grades, 4.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Vitreous floaters all grades, 4.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hyperbilirubinemia all grades, 54%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Vomiting all grades, 7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hypophosphatemia all grades, 9%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Dermatitis acneiform grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Dysgeusia grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Edema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Erythema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Exfoliative rash grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Eyelid edema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Face edema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Generalized rash grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hypogeusia grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Localized edema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Nausea grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Peripheral edema grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Pruritic rash grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash macular grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash maculo-papular grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash papular grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Rash grade 3-4, 0.7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Asthenia grade 3-4, 1.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Fatigue grade 3-4, 1.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hyperkalemia grade 3-4, 1.4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hypophosphatemia grade 3-4, 1.4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Blood creatinine increased grade 3-4, 3.9%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Acute kidney injury grade 3-4, 3.9%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Creatinine renal clearance decreased grade 3-4, 3.9%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Glomerular filtration rate decreased grade 3-4, 3.9%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Hyperbilirubinemia grade 3-4, 5%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Cardiac arrest grade 5, 1 patient
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Pneumonia grade 5, 1 patient
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 152
Health Status: unhealthy
Condition: ALK-positive NSCLC
Age Group: 56 years
Sex: M+F
Population Size: 152
Sources:
Back pain all grades, 12%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Dyspnea all grades, 16%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Headache all grades, 17%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Headache grade 3-4, 0.8%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Dyspnea grade 3-4, 3.17%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
Dyspnea grade 5, 1 patient
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56 years
n = 253
Health Status: unhealthy
Condition: ALK-positive non-small cell lung cancer
Age Group: 56 years
Sex: M+F
Population Size: 253
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 0.1 uM]
yes [IC50 0.9 uM]
yes [IC50 1.1 uM]
yes [IC50 >10 uM]
yes [IC50 >10 uM]
yes [IC50 >10 uM]
yes [IC50 >10 uM]
yes [IC50 >10 uM]
yes [Ki 2 uM]
unlikely (co-administration study)
Comment: Alectinib inhibits CYP2C8 in vitro, but simulations suggest that no clinically meaningful changes in repaglinide exposure would occur when it is coadministered with multiple doses of alectinib.
Page: -
yes
yes
yes
yes
yes
yes
yes
yes
no (co-administration study)
Comment: No dose adjustment is recommended for concomitant CYP3A4 substrates, because no clinically meaningful changes in midazolam exposure were observed when alectinib at a dose of 600 mg twice daily was coadministered with a single midazolam dose
Page: -
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer.
2007 Aug 2
KIF5B-ALK, a novel fusion oncokinase identified by an immunohistochemistry-based diagnostic system for ALK-positive lung cancer.
2009 May 1
CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
2011 May 17
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
2012 Feb 1
Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib.
2014 Nov 15
Perfect ALKemy: optimizing the use of ALK-directed therapies in lung cancer.
2014 Nov 15
Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance.
2014 Sep 1
Patents

Patents

Sample Use Guides

600 mg orally twice daily. Administer with food.
Route of Administration: Oral
Alectinib exhibited antiproliferative activity against SNU-2535 cells in vitro with IC50 of 33.1 nM.
Name Type Language
ALECTINIB
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
ALECTINIB [MI]
Common Name English
ALECTINIB [INN]
Common Name English
AF-802
Code English
ALECTINIB [WHO-DD]
Common Name English
RO-5424802
Code English
9-ETHYL-6,6-DIMETHYL-8-(4-(MORPHOLIN-4-YL)PIPERIDIN-1-YL)-11-OXO-6,11-DIHYDRO-5H-BENZO(B)CARBAZOLE-3-CARBONITRILE
Systematic Name English
ALECTINIB [USAN]
Common Name English
CH5424802
Code English
AF802
Code English
RO5424802
Code English
5H-BENZO(B)CARBAZOLE-3-CARBONITRILE, 9-ETHYL-6,11-DIHYDRO-6,6-DIMETHYL-8-(4-(4-MORPHOLINYL)-1-PIPERIDINYL)-11-OXO-
Systematic Name English
CH-5424802
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 462814
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
WHO-ATC L01XE36
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
NCI_THESAURUS C141136
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
Code System Code Type Description
EVMPD
SUB178557
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
LACTMED
Alectinib
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
IUPHAR
7739
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
PUBCHEM
49806720
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
RXCUI
1727455
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY RxNorm
ChEMBL
CHEMBL1738797
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
INN
9699
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
DRUG BANK
DB11363
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
EPA CompTox
1256580-46-7
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
FDA UNII
LIJ4CT1Z3Y
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
DRUG CENTRAL
4937
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
NCI_THESAURUS
C101790
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
NDF-RT
N0000175082
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY Kinase Inhibitors [MoA]
MERCK INDEX
M11898
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
CAS
1256580-46-7
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY
WIKIPEDIA
Alectinib
Created by admin on Sat Jun 26 09:52:11 UTC 2021 , Edited by admin on Sat Jun 26 09:52:11 UTC 2021
PRIMARY