Description of capmatinib

Capmatinib is an FDA-approved targeted drug for the treatment of adult patients with non-small cell lung cancer(NSCLC) whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping.Capmatinib inhibits the overactivity of c-Met, a receptor tyrosine kinase encoded by the MET proto-oncogene.Mutations in MET are involved in the proliferation of many cancers.

Mechanism of action

MET tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis, and angiogenesis; a variety of cancers (eg, lung, gastric) are associated when MET becomes dysregulated owing to MET amplifications and exon 14 skipping mutations. Capmatinib inhibits the phosphorylation of both wild-type and mutant variants of c-Met triggered by the binding of its endogenous ligand, hepatocyte growth factor - in doing so, it prevents c-Met-mediated phosphorylation of downstream signaling proteins, as well as the proliferation and survival of c-Met-dependent tumor cells.

side effects

The most common adverse reactions (≥20%) were edema (59%), nausea (46%), musculoskeletal pain (40%), fatigue (34%), vomiting (28%), dyspnea (25%), cough (21%), and decreased appetite (21%). The most common grade 3 adverse reactions (≥2%) were edema (13%), fatigue (8%), dyspnea (7%), pneumonia (6%), musculoskeletal pain (4.3%), nausea (2.4%), and vomiting (2.4%). Grade 4 dyspnea and pneumonia were reported in 0.5% of patients.