CAPMATINIB HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H17FN6O.2ClH.H2O
Molecular Weight	503.356
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=COWBUPJEEDYWKD-UHFFFAOYSA-N

InChI=1S/C23H17FN6O.2ClH.H2O/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;1H2

HIDE SMILES / InChI

Molecular Formula	C23H17FN6O
Molecular Weight	412.4191
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=666907
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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Hepatocyte growth factor receptor 56 Target ID: CHEMBL3717 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21918175	Inhibitor 8504		0.13 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Non-small cell lung cancer 211 Sources: https://clinicaltrials.gov/ct2/show/NCT02414139	Primary	Phase II 1147	Unknown Approved Use Unknown
Melanoma 88 Sources: https://clinicaltrials.gov/ct2/show/NCT02159066	Primary	Phase II 1147	Unknown Approved Use Unknown
Advanced hepatocellular carcinoma 3 Sources: https://clinicaltrials.gov/ct2/show/NCT02795429	Primary	Phase II 1147	Unknown Approved Use Unknown
Papillary renal cell carcinoma 3 Sources: https://clinicaltrials.gov/ct2/show/NCT02019693	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
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

Value	Dose	Co-administered	Analyte	Population
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY34099	https://www.001chemical.com/chem/1029712-80-8
AA Blocks	AA003A97	https://www.aablocks.com/goods/Goods/detail?id=AA003A97
Aaron Chemicals	AR003B0Z	http://www.aaronchem.com/1029712-80-8
abcr GmbH	AB460674	http://www.abcr.com/shop/en/AB460674
AbMole Bioscience	M2080	http://www.abmole.com/products/incb28060.html
Acadechem	ACDS-070219	http://www.acadechemical.com/product/144918
Acorn PharmaTech	ACN-050758	http://www.acornpharmatech.com/
Active Biopharma	ABP000812	http://www.activebiopharma.com/1029712-80-8
Adooq BioScience	A11132	https://www.adooq.com/incb28060.html
AK Scientific, Inc. (AKSCI)	Y0337	http://www.aksci.com/item_detail.php?cat=Y0337
Alsachim	4808	http://www.alsachim.com/product-C6188-glo.bal-view.html
Ambinter	Amb22170030	http://www.ambinter.com/reference/22170030
Angel Pharmatech	AG-10391	http://www.angelpharmatech.com/1029712-80-8.html
Angene	AGN-PC-04X71V	http://www.angenechemical.com/productshow/AGN-PC-04X71V.html
ApexBio Technology	A8448	http://www.apexbt.com/incb28060.html
Ark Pharm	AK174338	http://www.arkpharminc.com/products/1029712-80-8.html
Aurora Fine Chemicals LLC	K16.647.349	http://online.aurorafinechemicals.com/info?ID=K16.647.349
Aurum Pharmatech LLC	W-5775	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5775
BioChemPartner	BCP23444	http://www.biochempartner.com/1029712-80-8-BCP23444
BioCrick	BCC3793	http://www.biocrick.com/INCB28060-BCC3793.html
BioSynth	J-509516	https://www.biosynth.com/en/products/all-products/products/J-509516.html
Boerchem	BC261868	http://www.boerchem.com/?product_43039.html
Chem Scene	CS-1541	http://www.chemscene.com/1029712-80-8.html
Chemspace	CSSB00015189161	https://chem-space.com/CSSB00015189161
DC Chemicals	DC7167	http://www.dcchemicals.com/product_show-Capmatinib_INCB28060_.html
Debye Scientific	DA-33530	http://www.debyesci.com/cas_1029712-80-8.html
eNovation Chemicals	D372424	http://www.enovationchem.com/productDetails.asp?productID=D372424
Excenen	EX-A446	http://www.excenen.com/searchresultlist.php?id=1029712-80-8
Finetech	FT-0746310	http://www.finetechnology-ind.com/prod/detail/pub/1029712-80-8.html
Hairui	HR141090	http://www.hairuichem.com/en/product/1029712-80-8.html
Hefei Hirisun Pharmatech Co., Ltd	HR130870	http://hirisunpharm.com/1029712-80-8.html
iChemical	EBD2207157	http://www.ichemical.com/products/1029712-80-8.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01341861	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01341861
Matrix Scientific	145224	https://www.matrixscientific.com/145224.html
MedChem Express	HY-13404	https://www.medchemexpress.com/INCB28060.html
Molcore	MC34099	https://www.molcore.com/product/1029712-80-8
MuseChem	I000180	https://www.musechem.com/product/I000180.html
Renno Tech	RL00142	http://www.rennotech.com/product_show.asp?id=888
Selleck Chemicals	S2788	http://www.selleckchem.com/products/incb28060.html
Sinfoo Biotech	S054562	http://www.sinfoobiotech.com/product/1057960
Smolecule	S547925	http://www.smolecule.com/products/s547925
Smolecule	S746742	https://www.smolecule.com/products/s746742
Synblock Inc	SB16608	http://www.synblock.com/product/1029712-80-8.html
THE BioTek	bt-253455	https://www.thebiotek.com/product/inhibitors/bt-253455
THE BioTek	bt-287203	https://www.thebiotek.com/product/inhibitors/bt-287203
Yuhao Chemical	YH65244	http://www.chemyuhao.com/1029712-80-8.html

PubMed

Title	Date	PubMed
A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.	2011 Nov 15	21918175

Patents

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/ L inhibits c-MET more than 90%.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 16:31:31 GMT 2025` Edited by `admin` on `Tue Apr 01 16:31:31 GMT 2025`
Record UNII	C2A374O70X
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CAPMATINIB HYDROCHLORIDE

Official Name

English

CAPMATINIB DIHYDROCHLORIDE MONOHYDRATE

Preferred Name

English

Capmatinib hydrochloride monohydrate [WHO-DD]

Common Name

English

CAPMATINIB HYDROCHLORIDE HYDRATE [JAN]

Common Name

English

2-FLUORO-N-METHYL-4-(7-((QUINOLIN-6-YL)METHYL)IMIDAZO(1,2- B)(1,2,4)TRIAZIN-2-YL)BENZAMIDE DIHYDROCHLORIDE MONOHYDRATE

Systematic Name

English

CAPMATINIB HYDROCHLORIDE MONOHYDRATE

Common Name

English

BENZAMIDE, 2-FLUORO-N-METHYL-4-(7-(6-QUINOLINYLMETHYL)IMIDAZO(1,2-B)(1,2,4)TRIAZIN-2-YL)-, HYDROCHLORIDE, HYDRATE (1:2:1)

Systematic Name

English

CAPMATINIB HYDROCHLORIDE [USAN]

Common Name

English

CAPMATINIB HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

Capmatinib hydrochloride [WHO-DD]

Common Name

English

TABRECTA

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C129825