Definition

An orally bioavailable inhibitor of all members of the serine/threonine protein kinase Raf family, including A-Raf, B-Raf and C-Raf protein kinases, with potential antineoplastic activity. Upon oral administration, pan-RAF inhibitor JZP815 selectively binds to and inhibits the activity of wild-type and mutated forms of Raf, including B-Raf mutations, and B-Raf fusions. This prevents the activation of Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Oncogenic mutations in Raf plays a key role in the overactivation of the Ras-mitogen-activated protein kinase (MAPK) pathway and drives tumor cell proliferation and survival.