Basic Information
ID DDInter287
Drug Type small molecule
Molecular Formula C23H17FN6O
Molecular Weight 412.428
CAS Number 1029712-80-8
Description 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.[A199122] 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.[A199122] 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%.[A199122] 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,[L13380] for the treatment of NSCLC in patients whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping.[L13347] 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.[L13380] As this indication was granted under an accelerated approval, its continued approval is contingent upon verification of capmatinib's benefit in confirmatory trials.[L13347] Capmatinib was approved by Health Canada on June 8, 2022.[L42015]
ATC Classification L01EX17
IUPAC Name 2-fluoro-N-methyl-4-{7-[(quinolin-6-yl)methyl]imidazo[1,2-b][1,2,4]triazin-2-yl}benzamide
InChI LIOLIMKSCNQPLV-UHFFFAOYSA-N
Canonical SMILES CNC(=O)C1=C(F)C=C(C=C1)C1=NN2C(CC3=CC4=C(C=C3)N=CC=C4)=CN=C2N=C1
Useful Links DrugBank PubChem Substance ChemSpider BindingDB Wikipedia ChEMBL ZINC
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