ARQ 736

ARQ 736 is an orally bioavailable, highly soluble phosphate prodrug that acts as a potent and selective inhibitor of the B-raf (BRAF) protein kinase. It is designed for antineoplastic activity by targeting tumor cells harboring mutated BRAF alleles, particularly those with the V600E mutation. Upon administration, ARQ 736 is converted into its active form (ARQ 680) in the presence of phosphatases. The active metabolite selectively binds to and inhibits oncogenic B-raf, thereby potentially inhibiting proliferation of tumor cells with mutated BRAF genes. The drug was initially developed by ArQule and later acquired by Merck & Co for the treatment of solid tumors; however, clinical development was discontinued after phase I trials[1][3][4][5][7].