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CAPMATINIB HYDROCHLORIDE
CAS NO.: 1865733-40-9
Chemical Formula: C23H21Cl2FN6O2
Molecular Weight: 503.4000
DMF&GMP status: Please contact us for more details.
Description:
Capmatinib is an orally bioavailable inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor (HGFR)) with potential antineoplastic activity. 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.

Capmatinib is a small molecule kinase inhibitor targeted against c-Met (a.k.a. hepatocyte growth factor receptor [HGFR]), a receptor tyrosine kinase that, in healthy humans, activates signaling cascades involved in organ regeneration and tissue repair. Aberrant c-Met activation - via mutations, amplification, and/or overexpression - is known to occur in many types of cancer, and leads to overactivation of multiple downstream signaling pathways such as STAT3, PI3K/ATK, and RAS/MAPK. Mutations in MET have been detected in non-small cell lung cancer (NSCLC), and the prevalence of MET amplification in epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI)-naive patients with NSCLC has been reported to be 1.4% - 21%. This co-occurrence has made c-Met a desirable target in the treatment of NSCLC. Manufactured by Novartis and marketed under the brand name Tabrecta, capmatinib was granted accelerated approval by the FDA on May 6, 2020, for the treatment of NSCLC in patients whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping. The presence of the mutation must be confirmed by an FDA-approved test, such as the FoundationOne CDx assay (manufactured by Foundation Medicine, Inc.), which was approved by the FDA on the same day. As this indication was granted under an accelerated approval, its continued approval is contingent upon verification of capmatinib's benefit in confirmatory trials.

Capmatinib Hydrochloride is the hydrochloride salt form of capmatinib, an orally bioavailable inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor (HGFR)) with potential antineoplastic activity. 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.

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Approvals
Active Ingredient Dosage Form; Route Strength Proprietary Name Applicant
CAPMATINIB HYDROCHLORIDETABLET;ORALEQ 150MG BASETABRECTANOVARTIS PHARMACEUTICAL CORP
CAPMATINIB HYDROCHLORIDETABLET;ORAL EQ 200MG BASETABRECTANOVARTIS PHARMACEUTICAL CORP
Patent Data
Patent No. Patent Expiration Drug Substance Claim Drug Product Claim Patent Use Code
776767511/19/2027DSDP
842064506/05/2031DSDP
846133011/19/2027DSDP
890112305/20/2029U-2813
1059617805/20/2029DSDP
Exclusive Data
Exclusivity Code Exclusivity Expiration
NCE 05/06/2025
ODE-291 05/06/2027