The voltage-gated sodium channel NaV1.7 serves as a primary driver of action potential firing and neuronal excitability in the pain processing pathway. Genetic evidence supports the role of NaV1.7 in a range of inherited pain syndromes, both gain-of-function and loss-of-function. Consequently, there has been considerable interest in the development of an isoform-selective NaV1.7 inhibitor for the management of chronic neuropathic pain. This presentation will describe the strategic evolution of our program with a focus on the pharmacokinetic-pharmacodynamic relationship across multiple series of small molecule NaV1.7 inhibitors.

Strategic advances in the identification of small molecule inhibitors of NaV1.7 for the treatment of chronic pain

256th National Meeting (2018)

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