Characterization of Drug-Drug Interactions for Remdesivir, an Intravenous Antiviral for SARS-CoV-2, in Healthy Participants.

ABSTRACT: Remdesivir is an intravenous antiviral approved worldwide for the treatment of COVID-19 in adults and children. Remdesivir, as a prodrug inhibitor of RNA polymerase, undergoes intracellular activation to form the active metabolite along with 2 inactive circulating metabolites, GS-704277 and GS-441524. Based on drug-drug interaction (DDI) risks identified in vitro, three Phase 1 crossover DDI studies were conducted to evaluate remdesivir as a potential (i) object, (ii) inhibitor, or (iii) inducer of enzymes and transporters. As an object of organic anion transporting polypeptide (OATP) 1B1/1B3 and P-glycoprotein inhibition (cyclosporine A), remdesivir and GS-704277 exposures increased 2-fold and 3-fold, respectively, while GS-441524 was unchanged. Increased exposures were not clinically rel

SUBMITTER: Chang J 

PROVIDER: S-EPMC12610943 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature