VX-128 / Vertex - LARVOL DELTA

A phase I, randomized, double-blind, placebo-controlled, single- and multiple dose escalation study evaluating the safety, pharmacokinetics and pharmacodynamics of VX-128, a highly selective Na 1.8 inhibitor, in healthy adults. (PubMed, Clin Transl Sci) - "A trend in pain tolerance were observed for cold pressor- and pressure pain, which was dose-dependent for the latter. VX-128 was rapidly absorbed (median time to maximum plasma concentration between 1 and 2 h) with a half-life of ~80 h at 10 mg q.d., and approximately two-fold accumulation ratio after 10 and 30 mg q.d. Although VX-128, when given in a multiple dose fashion, resulted in early study termination due to tolerability issues, effects were observed on multiple pain tests that may support further investigation of Na 1.8 inhibitors as pain treatments."

Clinical • Journal • PK/PD data • Cardiovascular • Dermatology • Pain