How does capmatinib work?

Capmatinib is used to treat metastatic (cancer that has spread) non-small cell lung cancer in which the tumor has an abnormal mesenchymal-to-epithelial transition (MET) gene.

MET proteins belong to a family of enzymes called receptor tyrosine kinases, which are involved in cell growth. In non-small cell lung cancer patients with "METex14jumping", an abnormal form of the MET protein is produced, causing cancer cells to divide and grow in an uncontrolled manner. TabrectaThe active ingredient capmatinib is a receptor tyrosine kinase inhibitor that attaches to this abnormal MET protein in cancer cells. This blocks MET's action and helps slow the growth and spread of cancer.

The plasma protein binding rate of capmatinib is 96% and has nothing to do with the concentration of capmatinib . The apparent mean volume of distribution at steady state is164 L.

The blood to plasma ratio is 1.5 but decreases to 0.9 at higher concentrations. The effective elimination half-life of capmatinib is 6.5 hours. The mean steady-state apparent clearance (%CV) of capmatinib was 24liters/ hours (82%). Capmatinib is metabolized mainly through CYP3A4 and aldehyde oxidase. After a single oral administration of radiolabeled capmatinib to healthy subjects, 78%of the total radioactivity was recovered in the feces, 42% unchanged, and 22%of the total radioactivity was recovered unchanged and negligibly in the urine.

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