Safety, tolerability and pharmacokinetics of ASC10, a novel oral double prodrug of a broad-spectrum antiviral agent, ß-d-N4-hydroxycytidine: results from a randomized, double-blind, placebo-controlled phase 1 study in Chinese healthy subjects.
Expert Opin Investig Drugs
; : 1-10, 2024 Jul 12.
Article
en En
| MEDLINE
| ID: mdl-38988285
ABSTRACT
BACKGROUND:
Considering the rise of new SARS-CoV-2 variants that have reduced the efficacy of COVID-19 vaccines, the development of new antiviral medications for the disease has become increasingly necessary. In this study, ASC10, a novel antiviral prodrug, was studied in a phase 1 trial in healthy Chinese participants. RESEARCH DESIGN ANDMETHODS:
Part 1 involved 60 participants, receiving 50-800 mg ASC10 or placebo twice daily for 5.5 days. Part 2, with 12 participants, explored ASC10 dosing in the fed/fasting states.RESULTS:
ASC10-A, the main pharmacologically active metabolite, rapidly appeared in plasma (Tmax 1.00-2.00 h) and decreased (t1/2 1.10-3.04 h) without accumulation. The Cmax and area under the plasma concentration - time curve (AUC) of ASC10-A increased dose-dependently (50-800 mg BID) over 5.5 days, with no accumulation. The Tmax was slightly delayed in the fed state; however, the Cmax and AUC were similar between the fed and fasting states. Adverse events (AEs) were comparable (ASC10/placebo, 66.7%) and mostly mild (95%).CONCLUSION:
ASC10 was demonstrated to be safe and well tolerated and exhibited dose-proportional exposure and minimal food effects. CLINICAL TRIAL REGISTRATION www.clinicaltrials.gov identifier is NCT05523141.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
Expert Opin Investig Drugs
Asunto de la revista:
TERAPIA POR MEDICAMENTOS
Año:
2024
Tipo del documento:
Article
País de afiliación:
China