Drug intelligence / Profile preview

ibuzatrelvir

Development stage
Phase 3
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Ibuzatrelvir is an orally bioavailable, small-molecule antiviral drug developed by Pfizer for the treatment of COVID-19. It is a second-generation SARS-CoV-2 main protease (Mpro, also known as 3CL protease) inhibitor designed to improve upon nirmatrelvir by offering enhanced metabolic stability and oral bioavailability, thereby eliminating the need for coadministration with ritonavir. Ibuzatrelvir acts through reversible covalent inhibition of the viral Mpro enzyme, which is essential for processing viral polyproteins required for replication. This mechanism blocks viral replication in infected cells. The drug has demonstrated robust in vitro and clinical antiviral activity against SARS-CoV-2 and also potently inhibits MERS-CoV Mpro. Clinical trials have shown that ibuzatrelvir reduces viral load with an acceptable safety profile and low potential for drug-drug interactions[1][4][5][6][7].

Other names
ibuzatrelvir
02

Targets

MERS-CoV 3CLpro (MERS-CoV main protease)Mpro (3C-like proteinase of SARS-CoV-2)

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