ArQule

ArQule was a Nasdaq-listed (ARQL) biopharmaceutical company focused on kinase inhibitor discovery and development for cancer and rare diseases. Merck agreed on 9 December 2019 to acquire it for $20 a share in cash, an equity value of about $2.7 billion, and completed the acquisition on 16 January 2020, when ArQule became a wholly owned Merck subsidiary. The lead candidate, ARQ 531 (now nemtabrutinib), is an oral reversible inhibitor of wild-type and C481S-mutant BTK, then in Phase 2 for B-cell malignancies, with early activity in relapsed or refractory chronic lymphocytic leukaemia and Richter's transformation. The pipeline also included miransertib (ARQ 092), an AKT inhibitor in Proteus syndrome and PIK3CA-related overgrowth; ARQ 751, an AKT inhibitor in Phase 1 for solid tumours with AKT1 and PI3K mutations; and derazantinib, an FGFR-family inhibitor in a registrational trial for intrahepatic cholangiocarcinoma with Basilea and Sinovant. Atlas Venture lists ArQule as making cancer drugs using combinatorial chemistry.