Pharmacokinetics and Safety Study of HN0037, a Novel Anti‐Human Herpes Simplex Virus Inhibitor, in Healthy Volunteers

Abstract HN0037 is a helicase‐primase inhibitor developed to treat herpes simplex virus (HSV) infection. This study evaluated the safety, tolerability, and pharmacokinetics of HN0037, following oral administration in healthy volunteers. This double‐blind, placebo‐controlled, phase 1 study comprised two parts. In part 1, a single escalating dose of 10, 30, 60, 120, 200, 300, and 400 mg was assessed, and the food effect was evaluated in the 200‐mg cohort. In part 2, a multiple dose evaluation involving 30 and 100 mg once a day was conducted for 14 days. Following single oral doses, the systemic exposure of HN0037 increased in a proportional manner over the lower dose range (10–120 mg) and in a subproportional manner over the higher dose range (200–400 mg). Following multiple oral doses, significant drug accumulation of systemic exposure was found at steady state, and the half‐life ranged 50.4‐61.0 h. The food effect study results indicated that a high‐fat meal had a marginal impact on HN0037's pharmacokinetics. No differences were observed in the incidence of adverse events between HN0037 and placebo groups in either study. These results demonstrate that HN0037 is safe and well‐tolerated, supporting further clinical development.