Abstract
ArQule has agreed to be acquired by Merck & Co. for roughly $2.7 billion in cash, making it the latest small-molecule-focused cancer drug firm to be swallowed by big pharma. The deal, announced Dec. 9, centers on ARQ 531, a small molecule that inhibits Bruton’s tyrosine kinase (BTK), an enzyme that is crucial to the development and survival of B cells, a type of white blood cell. Although several BTK inhibitors are already on the market—notably AbbVie’s Imbruvica, which is on track to bring in more than $4 billion in sales this year, and BeiGene’s recently approved Brukinsa—there is room for more compounds. That’s because the approved drugs covalently bind to a cysteine residue on the signaling enzyme—a mechanism that works wonderfully until cancer cells mutate the residue. ARQ 531 is one of a handful of noncovalent BTK inhibitors in the clinic that are designed to overcome the resistance mechanism.
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