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News & Trends - Pharmaceuticals

MSD to acquire ArQule, advancing leadership in oncology

Health Industry Hub | December 11, 2019 |

MSD will acquire ArQule for an approximate equity value of $2.7 billion. ArQule is a publicly traded biopharmaceutical company focused on kinase inhibitor discovery and development for the treatment of patients with cancer and other diseases.

ArQule’s lead investigational candidate, ARQ 531, is a novel, oral Bruton’s tyrosine kinase (BTK) inhibitor currently in a Phase 2 dose expansion study for the treatment of B-cell malignancies.

“ArQule’s focus on precision medicine has yielded multiple clinical-stage oral kinase inhibitors that have novel and important properties,” said Dr. Roger M. Perlmutter, president, Merck Research Laboratories. “This acquisition strengthens Merck’s pipeline with the addition of these strategic assets including, most notably, ARQ 531, a compelling candidate for the treatment of B-cell malignancies.”

BTK inhibition has been shown to prevent B-cell receptor signaling that is critical for the survival and proliferation of leukemic cells in many B-cell malignancies. ARQ 531 is a highly selective, reversible inhibitor that blocks both wild-type BTK and the C481S mutant form of the enzyme that is commonly associated with resistance to other BTK inhibitors. In early clinical trials, ARQ 531 demonstrated a manageable safety profile and early signs of anti-tumor activity for the treatment of patients with relapsed or refractory chronic lymphocytic leukemia (CLL) and Richter’s Transformation. Final data from the Phase 1 study of ARQ 531 was presented on Dec. 9, 2019 at the 61st American Society of Hematology (ASH) Annual Meeting & Exposition in Orlando, Florida.

There are already BTK inhibitor class drugs on the market including Janssen/AbbVie’s Imbruvica (ibrutinib) and AstraZeneca’s Calquence (acalabrutinib).

The MSD transaction is expected to close early in the first quarter of 2020.

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