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oral CNS-penetrant AAK1 kinase inhibitor

in Ph. II for neuropathic pain

from high-throughput screen + opt.

J. Med. Chem.

Bristol-Myers Squibb, Wallingford, CT

oral CNS-penetrant AAK1 kinase inhibitor - Bristol-Myers Squibb, Wallingford, CT
4 mins read

Context. BMS-986176/LX-9211 (BMS) is an oral, CNS-penetrable AAK1 kinase inhibitor being developed for treatment of neuropathic pain. There are six main classes of pain medications, NSAIDs, opioids, ion channel modulators, serotonergic, monoaminergic, and GABAnergic drugs that are broadly used for pain in general, but neuropathic pain due to nerve damage or dysfunction is much harder to treat. Less than half of therapies achieve >50% pain reduction, while adverse effects are commonly associated with these drugs. BMS-986176/LX-9211 is a highly CNS-penetrant molecule with the potential to address a significant unmet need for patients with neuropathic pain. The drug was granted an FDA Fast Track designation in 2020. It is a rare example of a brain-penetrant kinase inhibitor outside of cancer (others…

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