What cancer does capmatinib treat?

Capmatinib (Capmatinib) is an oral small molecule inhibitor of the mesenchymal epithelial transition (MET) factor tyrosine kinase receptor that blocks the binding of its ligand hepatocyte growth factor (HGF), which usually activates signaling pathways involved in cell proliferation, movement and invasion. The MET gene is mutated or overexpressed in several human cancers, including lung, liver, breast and ovarian cancer, leading to uncontrolled cell growth and proliferation.

Capmatinib has potent activity against selected mutated forms of theMET receptor, including variants resulting from exon 14 skipping, and has been found to inhibit cancer cell growth in several tissue culture and animal models of MET-dysregulated cancers. In a moderately large open-label trial, capmatinib was found to induce objective responses in 41% of patients with refractory metastatic NSCLC harboring MET mutations and in a higher proportion of those treated.

Capmatinib was approved in the United States in 2020 for the treatment of adults with non-small cell lung cancer with documented mutations leading to MET exon 14 skipping, the first oncology drug approved for this indication. It is still being evaluated in other forms of cancer carrying MET mutations. Capmatinib is available in 150 and 200 mg tablets under the brand name Tabrecta. The recommended dose is 400 mg orally twice daily until disease progression or unacceptable toxicity.

Capmatinib side effects are common, occurring in nearly all patients treated, and about a quarter of patients have their dose adjusted or discontinued. Common side effects include edema, nausea and vomiting, anorexia, diarrhea or constipation, musculoskeletal pain, fatigue, fever, cough, dyspnea, and rash. Rare but potentially serious adverse events include pneumonitis, interstitial lung disease, hepatotoxicity, photosensitivity, hypersensitivity reactions, and embryo-fetal toxicity.