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

Details

Stereochemistry ACHIRAL
Molecular Formula C23H17FN6O.2ClH
Molecular Weight 485.3417
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CAPMATINIB HYDROCHLORIDE ANHYDROUS

SMILES

CN=C(c1ccc(cc1F)-c2cnc3ncc(Cc4ccc5c(cccn5)c4)n3n2)O.Cl.Cl

InChI

InChIKey=ZTNPHABKLIJXTL-UHFFFAOYSA-N
InChI=1S/C23H17FN6O.2ClH/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20;;/h2-9,11-13H,10H2,1H3,(H,25,31);2*1H

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C23H17FN6O
Molecular Weight 412.4199
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800031741

Capmatinib (INC280, INCB028060), is an orally bioavailable inhibitor of the proto-oncogene c-Met (hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. Novartis acquired Incyte's capmatinib, which is in Phase II clinical trial as monotherapy in patients with advanced hepatocellular carcinoma. Capmatinib selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.

CNS Activity

Curator's Comment:: INC280 is a highly potent and selective c-MET inhibitor which also penetrates the blood-brain barrier

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.13 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6450 ng/mL
400 mg 2 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CAPMATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
26300 ng × h/mL
400 mg 2 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CAPMATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.7 h
400 mg 2 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CAPMATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Other AEs: ALT increased, Nausea...
Other AEs:
ALT increased (grade 3-4, 13%)
Nausea (grade 1-2, 38%)
Vomiting (grade 1-2, 38%)
AST increased (grade 1-2, 25%)
Blood bilirubin increased (grade 1-2, 13%)
Fatigue (grade 1-2, 38%)
Decreased appetite (grade 1-2, 38%)
Peripheral edema (grade 1-2, 13%)
Hypoalbuminemia (grade 1-2, 13%)
Diarrhea (grade 1-2, 25%)
Protein total decreased (grade 1-2, 13%)
Stomatitis (grade 1-2, 13%)
Dyspepsia (grade 1-2, 13%)
Sources:
200 mg 2 times / day steady, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 5
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 5
Sources:
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
250 mg 2 times / day steady, oral
Studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 4
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 4
Sources:
DLT: Blood bilirubin increased...
Dose limiting toxicities:
Blood bilirubin increased (grade 3, 1 patient)
Sources:
450 mg 2 times / day steady, oral
Studied dose
Dose: 450 mg, 2 times / day
Route: oral
Route: steady
Dose: 450 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 9
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 9
Sources:
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Disc. AE: Peripheral edema, Pneumonitis...
AEs leading to
discontinuation/dose reduction:
Peripheral edema (all grades, 1.8%)
Pneumonitis (all grades, 1.8%)
Fatigue (all grades, 1.5%)
Peripheral edema (>2)
Blood creatinine increased (>2)
Nausea (>2)
Vomiting (>2)
Lipase increased (>2)
ALT increased (>2)
Dyspnea (>2)
Amylase increased (>2)
AST increased (>2)
Blood bilirubin increased (>2)
Fatigue (>2)
Pneumonia (>2)
Sources:
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
Disc. AE: Peripheral edema, Pneumonitis...
AEs leading to
discontinuation/dose reduction:
Peripheral edema (grade 3-4, 0.6%)
Pneumonitis (grade 3-4, 0.3%)
Fatigue (grade 3-4, 0.9%)
ALT increased (all grades, 0.9%)
ALT increased (grade 3-4, 0.6%)
AST increased (all grades, 0.9%)
AST increased (grade 3-4, 0.6%)
Sources: Page: p. 135
AEs

AEs

AESignificanceDosePopulation
Blood bilirubin increased grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Dyspepsia grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Hypoalbuminemia grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Peripheral edema grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Protein total decreased grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Stomatitis grade 1-2, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
AST increased grade 1-2, 25%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Diarrhea grade 1-2, 25%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Decreased appetite grade 1-2, 38%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Fatigue grade 1-2, 38%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Nausea grade 1-2, 38%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 1-2, 38%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
ALT increased grade 3-4, 13%
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 8
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 8
Sources:
Fatigue grade 3, 1 patient
DLT
200 mg 2 times / day steady, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 5
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 5
Sources:
Blood bilirubin increased grade 3, 1 patient
DLT
250 mg 2 times / day steady, oral
Studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 4
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 4
Sources:
Fatigue grade 3, 1 patient
DLT
450 mg 2 times / day steady, oral
Studied dose
Dose: 450 mg, 2 times / day
Route: oral
Route: steady
Dose: 450 mg, 2 times / day
Sources:
unhealthy, 56.0 years
n = 9
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Population Size: 9
Sources:
ALT increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
AST increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Amylase increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Blood bilirubin increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Blood creatinine increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Dyspnea >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Fatigue >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Lipase increased >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Nausea >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Peripheral edema >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Pneumonia >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Vomiting >2
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Fatigue all grades, 1.5%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Peripheral edema all grades, 1.8%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
Pneumonitis all grades, 1.8%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources:
ALT increased all grades, 0.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
AST increased all grades, 0.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
Pneumonitis grade 3-4, 0.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
ALT increased grade 3-4, 0.6%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
AST increased grade 3-4, 0.6%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
Peripheral edema grade 3-4, 0.6%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
Fatigue grade 3-4, 0.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 135
unhealthy, 71 years (range: 49 - 90 years)
n = 334
Health Status: unhealthy
Condition: Non-Small Cell Lung Cancer
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Population Size: 334
Sources: Page: p. 135
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
weak [Ki 0.9 uM]
likely
Comment: capmatinib was predicted to be a weak CYP2C8 inhibitor with 23% increase in Cmax and 39% increase in AUC of repaglinide
Page: 86, 88, 200, 202
yes [EC50 39.4 uM]
yes [Ki 0.28 uM]
yes [Ki 0.29 uM]
yes [Ki 3 uM]
unlikely
Comment: no significant exposure change was predicted for warfarin
Page: 86, 200, 202
yes [Ki 4.3 uM]
no (co-administration study)
Comment: In subjects with cancer, co-administration of midazolam (a sensitive CYP3A4 substrate) with multiple doses of capmatinib (400 mg b.i.d.) did not cause any clinically significant increase in midazolam exposure compared to administration of midazolam alone.
Page: 87, 200, 202
yes [Ki 6.1 uM]
unlikely
Comment: no significant exposure change was predicted for omeprazole
Page: 86, 200, 202
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: coadministration with rosuvastatin increased rosuvastatin AUC by 108% and Cmax by 204%
Page: 86, 88, 200
yes
yes (co-administration study)
Comment: coadministration with digoxin increased digoxin AUC by 47% and Cmax by 74%
Page: 86, 88
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
yes
yes (co-administration study)
Comment: itraconazole increased capmatinib exposure 42%; rifampicin decreased capmatinib exposure by 67% and Cmax by 56%
Page: 66, 75, 83, 85
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

400 mg twice every day by mouth, continuously
Route of Administration: Oral
Capmatinib inhibits c-MET phosphorylation with an IC50 value of approximately 1 nmol/L and a concentration of approximately 4 nmol/ L inhibits c-MET more than 90%.
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:30:41 UTC 2021
Edited
by admin
on Fri Jun 25 22:30:41 UTC 2021
Record UNII
Z0V2EW20JR
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CAPMATINIB HYDROCHLORIDE ANHYDROUS
Common Name English
BENZAMIDE, 2-FLUORO-N-METHYL-4-(7-(6-QUINOLINYLMETHYL)IMIDAZO(1,2-B)(1,2,4)TRIAZIN-2-YL)-, DIHYDROCHLORIDE
Systematic Name English
CAPMATINIB DIHYDROCHLORIDE
Common Name English
2-FLUORO-N-METHYL-4-(7-(QUINOLIN-6-YLMETHYL)IMIDAZO(1,2-B)(1,2,4)TRIAZIN-2-YL)BENZAMIDE DIHYDROCHLORIDE
Systematic Name English
Code System Code Type Description
PUBCHEM
44513225
Created by admin on Fri Jun 25 22:30:41 UTC 2021 , Edited by admin on Fri Jun 25 22:30:41 UTC 2021
PRIMARY
CAS
1029714-89-3
Created by admin on Fri Jun 25 22:30:41 UTC 2021 , Edited by admin on Fri Jun 25 22:30:41 UTC 2021
NON-SPECIFIC STOICHIOMETRY
CAS
1197376-85-4
Created by admin on Fri Jun 25 22:30:41 UTC 2021 , Edited by admin on Fri Jun 25 22:30:41 UTC 2021
PRIMARY
FDA UNII
Z0V2EW20JR
Created by admin on Fri Jun 25 22:30:41 UTC 2021 , Edited by admin on Fri Jun 25 22:30:41 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY