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Details

Stereochemistry ACHIRAL
Molecular Formula C23H17FN6O
Molecular Weight 412.4191
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CAPMATINIB

SMILES

CNC(=O)C1=CC=C(C=C1F)C2=NN3C(CC4=CC=C5N=CC=CC5=C4)=CN=C3N=C2

InChI

InChIKey=LIOLIMKSCNQPLV-UHFFFAOYSA-N
InChI=1S/C23H17FN6O/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)

HIDE SMILES / InChI

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
A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.
2011 Nov 15
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%.
Name Type Language
CAPMATINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
CAPMATINIB [USAN]
Common Name English
INCB-28060 FREE BASE
Code English
INC280
Code English
NVP-INC280
Code English
INC-280
Code English
Capmatinib [WHO-DD]
Common Name English
capmatinib [INN]
Common Name English
CAPMATINIB [MI]
Common Name English
INCB-28060
Code English
2-FLUORO-N-METHYL-4-(7-(QUINOLIN-6-YLMETHYL)IMIDAZO(1,2-B)(1,2,4)TRIAZIN-2-YL)BENZAMIDE
Systematic Name English
BENZAMIDE, 2-FLUORO-N-METHYL-4-(7-(6-QUINOLINYLMETHYL)IMIDAZO(1,2-B)(1,2,4)TRIAZIN-2-YL)-
Systematic Name English
NVP-INC280-NX
Code English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
FDA ORPHAN DRUG 644518
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
NCI_THESAURUS C1967
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
NCI_THESAURUS C1742
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C90564
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
CAS
1029712-80-8
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
SMS_ID
100000166975
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
FDA UNII
TY34L4F9OZ
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
WIKIPEDIA
Capmatinib
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
MERCK INDEX
m12204
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
EPA CompTox
DTXSID90145595
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
EVMPD
SUB181273
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
PUBCHEM
25145656
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
RXCUI
2362165
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
DAILYMED
TY34L4F9OZ
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
USAN
EF-10
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
ChEMBL
CHEMBL3188267
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
INN
9948
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY
DRUG BANK
DB11791
Created by admin on Sat Dec 16 17:08:00 GMT 2023 , Edited by admin on Sat Dec 16 17:08:00 GMT 2023
PRIMARY