capmatinib + selpercatinib

Capmatinib + selpercatinib is a combination of two targeted small molecule kinase inhibitors used in the treatment of non-small cell lung cancer (NSCLC) with specific genetic alterations. Capmatinib is a selective inhibitor of the MET receptor tyrosine kinase, approved for NSCLC patients with MET exon 14 skipping mutations and has demonstrated activity in cases with MET amplification. Selpercatinib is a highly selective RET kinase inhibitor, approved for NSCLC harboring RET fusions. This combination has been explored as a strategy to overcome acquired resistance to RET inhibition mediated by secondary MET amplification, which can occur after initial response to RET inhibitors like selpercatinib. The dual inhibition targets both the primary oncogenic driver (RET fusion) and the resistance pathway (MET amplification), offering potential benefit in overcoming resistance mechanisms in advanced lung cancer[1][2][3].

Brand names

Tabrecta (capmatinib)Retevmo (selpercatinib)

Other names

capmatinib and selpercatinib combination