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DS-5058b is an orally bioavailable small molecule developed by Daiichi Sankyo that acts as a selective inhibitor of the voltage-gated sodium channel Nav1.7 (encoded by the SCN9A gene). Nav1.7 is a key mediator of pain signaling in the peripheral nervous system, and its selective inhibition is a sought-after strategy for treating chronic and neuropathic pain while avoiding the side effects associated with non-selective sodium channel blockers, such as Nav1.5 in the heart or Nav1.1 and Nav1.2 in the central nervous system. DS-5058b has been evaluated in Phase 1 clinical trials to assess its safety, tolerability, and pharmacokinetics in healthy volunteers, specifically targeting indications related to neuropathic and chronic pain.
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