Pharmacokinetics, Tolerability, and Safety of Glecaprevir/Pibrentasvir Co‐formulated Bilayer Tablet Following Repeated Administration in Healthy Chinese Adults

Abstract

Glecaprevir (GLE)/pibrentasvir (PIB) is an all‐oral, interferon‐ and ribavirin‐free, pan‐genotypic fixed‐dose combination regimen approved for the treatment of all major genotypes of hepatitis C virus (HCV) infection in many countries worldwide. To support clinical development in China, an open‐label, single‐center phase 1 study was conducted to evaluate the pharmacokinetics, safety, and tolerability of GLE/PIB in healthy Chinese adults in Mainland China. Eighteen participants received 3 tablets of coformulated GLE/PIB 100/40 mg once daily (QD) for 7 days. Following GLE/PIB 300 mg/120 mg administration, GLE and PIB reached maximum concentration in 4‐5 hours with a terminal elimination half‐life of 5.9 and 25 hours, respectively. Both GLE and PIB reached steady state by day 5, with no‐to‐minimal accumulation (≤17% higher). GLE/PIB exposures in healthy Chinese participants were similar to historical observations across phase 1 studies in healthy Western participants. GLE/PIB was safe and well‐tolerated, with most adverse events being mild. These pharmacokinetics and safety data, together with existing global efficacy and safety data in healthy and HCV‐infected Western participants, support the use of GLE/PIB 300 mg/120 mg QD in adult Chinese patients with chronic HCV infection.