Drug intelligence / Profile preview

obeldesivir

Development stage
Phase 3
Lead developer
Gilead Sciences
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Obeldesivir is an oral nucleoside analog prodrug developed to inhibit the RNA-dependent RNA polymerase of SARS-CoV-2 and other viral polymerases. It is an isobutyric ester prodrug of GS-441524, designed to improve the oral bioavailability of its parent nucleoside. Once administered, obeldesivir is hydrolyzed to GS-441524, which is then converted intracellularly into remdesivir-triphosphate (GS-443902), a bioactive ATP analogue with broad-spectrum antiviral activity. This active metabolite inhibits viral replication by targeting viral RNA polymerases. Obeldesivir demonstrates improved pharmacokinetics compared to its parent compound and can be administered orally, unlike remdesivir which requires intravenous administration. The drug has shown promising results in preclinical models and clinical trials for COVID-19 treatment in high-risk outpatients, with a favorable safety profile and low potential for clinically significant drug-drug interactions[1][3][5][6][8].

Other names
GS-5245GS5245GS 5245ATV006ATV-006ATV 006
02

Targets

RdRp (Coronavirus RNA-dependent RNA polymerase)

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