Drug intelligence / Profile preview

olgotrelvir

Development stage
Phase 3
Lead developer
ACEA Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Olgotrelvir (STI-1558) is a novel oral antiviral drug developed as a dual inhibitor targeting both the SARS-CoV-2 main protease (Mpro), an essential enzyme for viral replication, and human cathepsin L (CTSL), a host protease involved in viral entry into cells[1][3][6]. Olgotrelvir is administered as a prodrug that is converted in plasma to its active form, AC1115[7][8]. This dual mechanism of action—blocking both virus replication and entry—aims to enhance antiviral efficacy and reduce the risk of resistance. Olgotrelvir has demonstrated potent activity against multiple SARS-CoV-2 variants, including those resistant to other antivirals such as Paxlovid. Clinical trials have shown that it significantly accelerates symptom recovery and reduces viral load in nonhospitalized patients with mild-to-moderate COVID-19, with a favorable safety profile[3][4]. The drug was developed by Sorrento Therapeutics/ACEA Therapeutics.

Brand names
Ovydso
Other names
olgotrelvir sodium
02

Targets

CTSL (Cathepsin L)Mpro (3C-like proteinase of SARS-CoV-2)

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