ArQule, Inc. (NASDAQ: ARQL) today announced the commencement of patient dosing in a Phase 1 clinical trial with ARQ 736, a small molecule inhibitor of the RAF kinases.
ARQ 736 is an ATP-competitive pan-RAF kinase inhibitor discovered and developed at ArQule. This compound has been shown pre-clinically to be a potent inhibitor of mutant BRAF (V600E), wild-type BRAF and c-RAF.
The primary objective of this trial is to assess the safety and tolerability of ARQ 736 in patients with advanced solid tumors that contain BRAF mutations. Additional objectives include assessment of pharmacokinetic and pharmacodynamic profiles in cancer patients, as well as preliminary evidence of anti-tumor activity and a recommended Phase 2 dose.