Article ; Online: Olgotrelvir, a dual inhibitor of SARS-CoV-2 M
Med (New York, N.Y.)
2024 Volume 5, Issue 1, Page(s) 42–61.e23
Abstract: Background: Oral antiviral drugs with improved antiviral potency and safety are needed to address current challenges in clinical practice for treatment of COVID-19, including the risks of rebound, drug-drug interactions, and emerging resistance.: ... ...
| Abstract | Background: Oral antiviral drugs with improved antiviral potency and safety are needed to address current challenges in clinical practice for treatment of COVID-19, including the risks of rebound, drug-drug interactions, and emerging resistance. Methods: Olgotrelvir (STI-1558) is designed as a next-generation antiviral targeting the SARS-CoV-2 main protease (M Findings: Olgotrelvir is a highly bioavailable oral prodrug that is converted in plasma to its active form, AC1115. The dual mechanism of action of olgotrelvir and AC1115 was confirmed by enzyme activity inhibition assays and co-crystal structures of AC1115 with SARS-CoV-2 M Conclusions: Olgotrelvir is an oral inhibitor targeting M Funding: Funded by Sorrento Therapeutics. |
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| MeSH term(s) | Animals ; Humans ; Mice ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Cathepsin L/antagonists & inhibitors ; COVID-19/prevention & control ; Disease Models, Animal ; Mice, Transgenic ; SARS-CoV-2 ; Coronavirus Protease Inhibitors/chemistry ; Coronavirus Protease Inhibitors/pharmacology ; Coronavirus 3C Proteases/antagonists & inhibitors ; COVID-19 Drug Treatment/methods |
| Chemical Substances | Antiviral Agents ; Cathepsin L (EC 3.4.22.15) ; STI-1558 ; Coronavirus Protease Inhibitors ; Coronavirus 3C Proteases (EC 3.4.22.28) |
| Language | English |
| Publishing date | 2024-01-04 |
| Publishing country | United States |
| Document type | Journal Article |
| ISSN | 2666-6340 |
| ISSN (online) | 2666-6340 |
| DOI | 10.1016/j.medj.2023.12.004 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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