Ensitrelvir as a potential treatment for COVID-19.

Abstract

INTRODUCTION:

First-generation therapeutics have improved clinical outcomes in patients infected with SARS-CoV-2. However, viral evolution has produced variants and subvariants capable of resisting many of these drugs and novel treatment strategies are urgently needed.

AREAS COVERED:

A corporate compound library screen identified ensitrelvir (formerly S-217622), a non-covalent, non-peptidic, orally bioavailable small-molecule protease inhibitor as a potential treatment for SARS-CoV-2. Ensitrelvir cleaves the active site of the 3C-like protease (3CLpro), which is conserved across SARS-CoV-2 variants and subvariants, with no human cell protease with similar specificity.

EXPERT OPINION:

Ensitrelvir demonstrates strong in vitro antiviral activity against the SARS-CoV-2 Omicron subvariants BA.4 and BA.5, which have driven new waves of infection throughout 2022, suggesting a potential therapeutic option for patients with COVID-19. This manuscript reviews what is known about ensitrelvir and explores how this drug may be used in the future to address the SARS-CoV-2 pandemic.

• Authors: Matthew W McCarthy
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 23 Issue 18 Pg. 1995-1998 (Dec 2022) ISSN: 1744-7666 [Electronic] England
• PMID: 36350029 (Publication Type: Journal Article)

Chemical References

• Viral Nonstructural Proteins
• Cysteine Endopeptidases
• Protease Inhibitors
• Antiviral Agents

Topics

• Humans
• SARS-CoV-2
• Viral Nonstructural Proteins (chemistry)
• Cysteine Endopeptidases (chemistry)
• Protease Inhibitors (pharmacology, therapeutic use)
• Antiviral Agents (pharmacology, therapeutic use, chemistry)
• COVID-19 Drug Treatment