Capmatinib hydrochlorideProduct ingredient for Capmatinib
- Name
- Capmatinib hydrochloride
- Drug Entry
- Capmatinib
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.2 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.2 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%.2 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, 2020,4 for the treatment of NSCLC in patients whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping.3 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.4 As this indication was granted under an accelerated approval, its continued approval is contingent upon verification of capmatinib's benefit in confirmatory trials.3 Capmatinib was approved by Health Canada on June 8, 2022.7
- Accession Number
- DBSALT002950
- Structure
- Synonyms
- Capmatinib dihydrochloride monohydrate / Capmatinib HCl / Capmatinib hydrochloride / Capmatinib hydrochloride hydrate
- External IDs
- NVP-INC280-AAA
- UNII
- C2A374O70X
- CAS Number
- 1865733-40-9
- Weight
- Average: 503.36
Monoisotopic: 502.1087075 - Chemical Formula
- C23H21Cl2FN6O2
- InChI Key
- COWBUPJEEDYWKD-UHFFFAOYSA-N
- InChI
- 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
- IUPAC Name
- 2-fluoro-N-methyl-4-{7-[(quinolin-6-yl)methyl]imidazo[1,2-b][1,2,4]triazin-2-yl}benzamide hydrate dihydrochloride
- SMILES
- O.Cl.Cl.CNC(=O)C1=C(F)C=C(C=C1)C1=NN2C(CC3=CC4=C(C=C3)N=CC=C4)=CN=C2N=C1
- External Links
- ChemSpider
- 58791261
- ChEMBL
- CHEMBL3989937
- Wikipedia
- Capmatinib
- Predicted Properties
Property Value Source Water Solubility 0.00529 mg/mL ALOGPS logP 3.04 ALOGPS logP 2.96 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 12.77 Chemaxon pKa (Strongest Basic) 4.55 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 85.07 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 125.27 m3·mol-1 Chemaxon Polarizability 42.1 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon