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Pharmacology and Mechanism of Action of Suzetrigine, a Potent and Selective Na<sub>V</sub>1.8 Pain Signal Inhibitor for the Treatment of Moderate to Severe Pain.


ABSTRACT:

Introduction

There is a high unmet need for safe and effective non-opioid medicines to treat moderate to severe pain without risk of addiction. Voltage-gated sodium channel 1.8 (NaV1.8) is a genetically and pharmacologically validated pain target that is selectively expressed in peripheral pain-sensing neurons and not in the central nervous system (CNS). Suzetrigine (VX-548) is a potent and selective inhibitor of NaV1.8, which has demonstrated clinical efficacy and safety in multiple acute pain studies. Our study was designed to characterize the mechanism of action of suzetrigine and assess both nonclinical and clinical data to test the hypothesis that selective NaV1.8 inhibition translates into clinical efficacy and safety, including lack of addict

SUBMITTER: Osteen JD 

PROVIDER: S-EPMC11914629 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature