Phase 1 Evaluation of VH4524184, a Third-Generation Integrase Strand Transfer Inhibitor With an Enhanced Resistance Profile.

ABSTRACT:

Background

Integrase strand transfer inhibitors (INSTIs) have been fundamental to human immunodeficiency virus type 1 (HIV-1) treatment for over 15 years. VH4524184 (VH-184) is a third-generation INSTI with long-acting potential currently in development for HIV-1 treatment.

Methods

This double-blind, randomized, placebo-controlled, phase 1, first-time-in-human (FTIH) study evaluated oral VH-184 in adults without HIV-1 administered as single ascending doses (10-460 mg; part 1), multiple ascending doses (160-480 mg) for 14 days with concomitant midazolam (480 mg cohort; part 2), and as a single dose (100 mg) under fasted/fed conditions (part 3) to assess safety, tolerability, and pharmacokinetics. VH-184 resistance was evaluated in vitro against pseudotyped viruses containing

SUBMITTER: Rogg L 

PROVIDER: S-EPMC12497951 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature