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

Details

Stereochemistry ACHIRAL
Molecular Formula C23H17FN6O
Molecular Weight 412.4199
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CAPMATINIB

SMILES

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

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
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

CNS Penetrant
2415
Curator's Comment:: INC280 is a highly potent and selective c-MET inhibitor which also penetrates the blood-brain barrier

Originator

Approval Year

2020
91
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
7701
Non-small cell lung cancer
Melanoma
Advanced hepatocellular carcinoma
Papillary renal cell carcinoma
 0.130000000000000004 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Hepatocyte growth factor receptor
Phase II
Primary
Hepatocyte growth factor receptor
Phase II
Primary
Hepatocyte growth factor receptor
Phase II
Primary
Hepatocyte growth factor receptor
Phase II
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6450 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/30724423
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
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/30724423
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
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/30724423
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
DLT: Blood bilirubin increased...
Dose limiting toxicities:
Blood bilirubin increased (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://pubmed.ncbi.nlm.nih.gov/31778267
unhealthy, 56.0 years
Health Status: unhealthy
Age Group: 56.0 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31778267
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213591s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
unhealthy, 71 years (range: 49 - 90 years)
Health Status: unhealthy
Age Group: 71 years (range: 49 - 90 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213591Orig1s000MultidisciplineR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1470
inhibitor
1318

inducer
343
inhibitor
1360

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
761

CYP2C19
1215

P-gp
1089

OCT1
473

OAT1
547

OAT3
570

OATP1B1
698

BCRP
574

MATE1
290

MATE2
258

CYP3A
175

OATP1B3
613

BSEP
363

MRP2
341
aldehyde oxidase
15

P-gp
1223
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2C8
810
 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
CYP2C9
1362
 yes [EC50 39.4 uM]
MATE1
291
 yes [Ki 0.28 uM]
MATE2
258
 yes [Ki 0.29 uM]
CYP2C9
1362
 yes [Ki 3 uM]
unlikely
Comment: no significant exposure change was predicted for warfarin
Page: 86, 200, 202
CYP3A
244
 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
CYP2C19
1277
 yes [Ki 6.1 uM]
unlikely
Comment: no significant exposure change was predicted for omeprazole
Page: 86, 200, 202
BSEP
364
 yes
CYP2C8
810
 yes
CMN288
3
CYP2C9
1362
 yes
CMN288
3
CYP3A
244
 yes
CMN288
3
MRP2
421
 yes
OAT1
551
 yes
OAT3
572
 yes
OATP1B1
713
 yes
OATP1B3
622
 yes
OCT1
488
 yes
BCRP
639
 yes
yes (co-administration study)
Comment: coadministration with rosuvastatin increased rosuvastatin AUC by 108% and Cmax by 204%
Page: 86, 88, 200
P-gp
1255
 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
P-gp
1223
 yes
aldehyde oxidase
15
 yes
CYP3A4
1470
 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
hERG
1392
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY34099
1PlusChem LLC
1P003ASN
AChemBlock
K12247
AChemBlock
L21782
AK Scientific
Y0337
AOBIOUS INC
AOB87335
APExBIO
A8448
AbovChem LLC
HY-13404
Ambeed
A193720
Angene
AGN-PC-04X71V
AstaTech
41353
BLDpharm
BD304056
BOC Sciences
1029712-80-8
BlocksMatrix Scientific
145224
Cayman Chemical
20056
Chem Scene
CS-1541
ChemShuttle
104838
ChemShuttle
141002
Compound Cloud
122201352
Compound Cloud
25145656
Debye Scientific
DA-33530
Excenen
EX-A446
Hairui
HR141090
Hangzhou APIChem Technology
AC-25890
Hangzhou Yuhao Chemical Technology
YH65244
KeyOrganics
AS-74142
Lan Pharmatech
LQT-B42882
MedChem Express
HY-13404
MolPort
MolPort-023-293-554
MolPort
MolPort-046-423-267
Molcore
MC34099
Molnova
M10142
Molnova
M17871
Norris Pharm
NSZB-A233768
Ryan Scientific
UNC0379
ShangHai Biochempartner
BCP25379
TargetMol
T1963
TargetMol
T4260
ZINC
ZINC000043195321
http://zinc15.docking.org/substances/ZINC000043195321
eMolecules
114309411
eMolecules
168893710
eMolecules
44786187
eNovation Chemicals
D572848
mcule
MCULE-1762412645
mcule
MCULE-8719661234
PubMed

PubMed

TitleDatePubMed
Patents

Patents

08420645
3
20080167287
3
20090291956
3
20110136781
3
20130289036
3

Sample Use Guides

In Vivo Use Guide
400 mg twice every day by mouth, continuously
Route of Administration: Oral
In Vitro Use Guide
Capmatinib inhibits c-MET phosphorylation with an IC50 value of approximately 1 nmol/L and a concentration of approximately 4 nmol/
Substance Class Chemical
Created
by admin
on Sat Jun 26 08:57:27 UTC 2021
Edited
by admin
on Sat Jun 26 08:57:27 UTC 2021
Record UNII
TY34L4F9OZ
Record Status Validated (UNII)
Record Version
  • Download
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
CAPMATINIB [WHO-DD]
Common Name English
NVP-INC280
Code English
INC-280
Code English
CAPMATINIB [INN]
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 Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
NCI_THESAURUS C1742
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
FDA ORPHAN DRUG 644518
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C90564
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
CAS
1029712-80-8
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
FDA UNII
TY34L4F9OZ
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
EPA CompTox
1029712-80-8
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
EVMPD
SUB181273
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
PUBCHEM
25145656
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
RXCUI
2362165
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
ChEMBL
CHEMBL3188267
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
INN
9948
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
DRUG BANK
DB11791
Created by admin on Sat Jun 26 08:57:28 UTC 2021 , Edited by admin on Sat Jun 26 08:57:28 UTC 2021
PRIMARY
Related Record Type Details
MULTIDRUG AND TOXIN EXTRUSION PROTEIN 2-K
TRANSPORTER -> INHIBITOR
REVERSIBLE
Structure of CAPMATINIB
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
MULTIDRUG AND TOXIN EXTRUSION PROTEIN 1
TRANSPORTER -> INHIBITOR
REVERSIBLE
Structure of CAPMATINIB
EXCRETED UNCHANGED
TRACE AMOUNT
URINE
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
independent of capmatinib concentration
BINDING
Structure of CAPMATINIB HYDROCHLORIDE
SALT/SOLVATE -> PARENT
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Structure of CAPMATINIB HYDROCHLORIDE ANHYDROUS
SALT/SOLVATE -> PARENT
ALDEHYDE OXIDASE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of CMN-290
METABOLITE -> PARENT
PLASMA
Structure of CNJ-294
METABOLITE -> PARENT
URINE
Structure of CJH-800
METABOLITE -> PARENT
FECAL; PLASMA; URINE
Structure of CMN-288
METABOLITE -> PARENT
URINE
Structure of CJK-530
METABOLITE -> PARENT
FECAL; PLASMA; URINE
Structure of CMC-583
METABOLITE -> PARENT
PLASMA
Structure of CMN-288
METABOLITE -> PARENT
FECAL
Structure of CMC-583
METABOLITE -> PARENT
MINOR
FECAL; URINE
Structure of CMN-288
METABOLITE -> PARENT
MAJOR
PLASMA
Structure of CNJ-294
METABOLITE -> PARENT
PLASMA
Structure of CNN-019
METABOLITE -> PARENT
Structure of CMN-290
METABOLITE -> PARENT
MINOR
FECAL; URINE
Related Record Type Details
Structure of CAPMATINIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC IN PATIENTS WITH CANCER

ORAL ADMINISTRATION

blood-to-plasma ratio PHARMACOKINETIC at higher concentrations

blood-to-plasma ratio PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC AT STEADY-STATE

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