Vixotrigine (BIIB074): A Comprehensive Monograph on a Novel Voltage-Gated Sodium Channel Blocker for Neuropathic Pain

Executive Summary

Vixotrigine (DB11706), also known by its development codes BIIB074, CNV1014802, and GSK-1014802, is an investigational, orally administered small molecule developed for the treatment of chronic neuropathic pain. Originating at GlaxoSmithKline and advanced through Convergence Pharmaceuticals before its acquisition by Biogen, Vixotrigine was engineered to address the significant tolerability limitations of existing voltage-gated sodium channel (Nav) blockers, such as carbamazepine. Its core pharmacological feature is a state- and use-dependent mechanism of action, designed to selectively inhibit pathologically hyperexcitable neurons characteristic of pain states while sparing normal physiological nerve signaling. This approach was intended to deliver targeted analgesia with a superior safety profile.

From a physicochemical and pharmacokinetic standpoint, Vixotrigine was an exemplary drug candidate. It possesses favorable "drug-like" properties, adheres to Lipinski's Rule of Five, and exhibits a predictable pharmacokinetic profile with rapid absorption, a half-life of approximately 11 hours suitable for twice-daily dosing, and linear kinetics without the autoinduction that complicates the use of older agents. Clinical studies consistently affirmed its primary strategic goal: Vixotrigine was generally well-tolerated across a range of doses, with a manageable side-effect profile consisting primarily of mild-to-moderate, transient central nervous system effects like dizziness and headache.