Merck Successfully Completes The Acquisition Of ArQule And Obtains A New Generation Of BTK Inhibitor ARQ 531

- Jan 30, 2020-


Merck & Co has announced that it has successfully completed the acquisition of ArQule. The acquisition was announced on December 9, 2019. Merck, through a subsidiary, acquired all publicly issued shares of ArQule for US $ 20 per share for a total purchase amount of approximately US $ 2.7 billion. During the acquisition, Merck's subsidiary was merged into ArQule, which became a wholly-owned subsidiary of Merck.

ArQule focuses on the discovery and development of kinase inhibitors for the treatment of cancer and other diseases. The company's main drug candidate is ARQ 531, a new, oral, reversible Bruton tyrosine kinase (BTK) inhibitor capable of inhibiting wild-type BTK and C481S mutant BTK. The C481S mutation is a known resistance mechanism of the first generation of irreversible BTK inhibitors. Currently, ARQ 531 is in a phase II dose extension study for B-cell malignancies that have failed to treat other therapies.

At the 2019 American Society of Hematology (ASH) Annual Meeting, ArQule announced data from Phase I clinical trials of ARQ 531: 47 patients with relapsed / refractory B-cell malignancies received different doses (5, 10, 15, 20, 30, 45, 65, 75 mg, once daily) ARQ531 treatment. Of the 9 patients with relapsed / refractory chronic lymphocytic leukemia (CLL) who received a once-daily dose of ≥65 mg and whose efficacy was evaluated, 8 patients achieved partial response (PR) with an overall response rate (ORR) of 89%. In particular, 8 of the 9 patients with evaluable CLL carried the BTK-C481S mutation, and 7 of them had partial remission.

In addition to ARQ 531, there are several other assets in the ArQule pipeline, including: (1) miransertib (ARQ 092), which is a potent and selective AKT serine / threonine kinase inhibitor, currently an I / Phase II clinical trial (NCT03094832) is enrolling patients, including patients with Proteus syndrome and patients with PIK3CA-related overgrowth disease profile (PROS); (2) ARQ751, a new generation of powerful and selective AKT inhibitors, currently A Phase I clinical trial (NCT02761694) is enrolling patients, specifically patients with solid tumors carrying PKD3CA / AKT / PTEN mutations; (3) derazantinib, a pan-FGFR (fibroblast growth factor receptor) inhibitor Agent, currently in Phase I / II clinical treatment, for the treatment of FGFR-driven intrahepatic cholangiocarcinoma (iCCA) and other cancers.

Dr. Roger M. Perlmutter, President of Merck Research Laboratories, previously stated, "ArQule's focus on precision medicine has resulted in multiple clinical stages of oral kinase inhibitors that have novel and important properties. This acquisition will increase these strategic assets Will strengthen Merck's pipeline, most notably ARQ 531, a powerful drug candidate for the treatment of B-cell malignancies. "(from,compile