RAF inhibitor BDTX-4933

A central nervous system (CNS)-penetrant inhibitor of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon oral administration, BDTX-4933 selectively targets, binds to and inhibits the activity of activated RAF that results from BRAF monomeric (class I), and dimeric class II (Ras-independent) and class III (Ras-dependent) mutations, and RAS mutations, which may inhibit the proliferation of tumor cells expressing a mutated BRAF, KRAS or NRAS gene. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival. BRAF, a serine/threonine protein kinase, plays a key role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. Ras serves an important role in cell signaling, division and differentiation. Mutations of Ras may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.