naporafenib

Naporafenib is an orally available, investigational small molecule inhibitor that targets all members of the serine/threonine protein kinase Raf family (pan-Raf inhibitor). By binding to and inhibiting Raf proteins, naporafenib disrupts the Raf-mediated signal transduction pathways—specifically the MAPK pathway—which are often overactive in cancer cells. This inhibition leads to reduced proliferation and survival of tumor cells with upregulated or mutated Ras/Raf/MEK/ERK signaling. Naporafenib is being developed primarily for advanced or metastatic solid tumors harboring RAS Q61X mutations and NRAS-mutant melanoma. It has been studied both as a single agent and in combination with trametinib (a MEK1/2 inhibitor) to enhance antitumor efficacy by blocking multiple points in the MAPK pathway. The drug has received FDA Fast Track Designation for unresectable or metastatic NRAS-mutant melanoma.

Brand names

naporafenib

Other names

naporafenib [INN]