ARQ-680

ARQ-680 is a potent, small molecule pan-RAF kinase inhibitor that targets BRAF, mutant BRAF(V600E), and CRAF. It serves as the active moiety of the phosphate prodrug ARQ-736. Developed by ArQule (now a subsidiary of Merck & Co.), ARQ-680 works by binding to mutated B-RAF protein kinases and blocking abnormal signaling through the MAPK/ERK pathway, which is a key driver in various malignancies. This inhibition leads to the suppression of tumor cell growth and the induction of apoptosis. ARQ-680 has been investigated in clinical trials for the treatment of advanced solid tumors harboring BRAF mutations, such as metastatic melanoma and colorectal cancer. Although it reached early clinical development, it is no longer listed in the active pipelines of its developers.