Approved and Clinical-Stage RAF Inhibitors

The RAF family kinase plays a crucial role as a pivotal component within the RAS/RAF/MEK/ERK signaling pathway, which is a fundamental cellular pathway involved in various physiological processes. Deregulation in RAF kinases, with a particular emphasis on BRAF, are frequently observed in malignant conditions including melanomas and papillary thyroid cancers. Consequently, the targeted inhibition of RAF kinases has become as a prominent focus in drug discovery efforts, with notable success. To date, six RAF inhibitors have received regulatory approval for the treatment of diverse cancers, while an additional ten inhibitors have been or are currently undergoing clinical trials, underscoring the ongoing exploration and development of novel therapeutic options in this area.

Approved and Clinical-Stage RAF Inhibitors