13 minute read
Feb. 28, 2024

NaV1.8 Inhibitor Roundup: From Abbott to Vertex

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NaV1.8, a member of the voltage-gated sodium channel (NaV) family, is predominantly expressed in peripheral sensory neurons. Based on rodent NaV1.8 knockout and knockdown studies and a 2012 report of gain-of-function mutations in humans, NaV1.8 has been linked to nociceptive, inflammatory, and neuropathic pain, including chronic neuropathic pain. Due to their early contributions in the mid-2000s, Abbott, Icagen, and Pfizer are recognized as early pioneers in the NaV1.8 inhibitor arena. Despite these discovery efforts, the translation of promising preclinical compounds into efficacious clinical candidates remained unrealized. VX-548 is now a notable exception, representing the only NaV1.8 inhibitor to achieve success in Ph. III clinical trials across various pain conditions. This compound roundup provides a historical recap of both preclinical and clinical NaV1.8 inhibitors that shaped the landscape for the new era of pain management we are witnessing today.

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