An oral SARS-CoV-2 M<sup>pro</sup> inhibitor clinical candidate for the treatment of COVID-19.
rct · Level II
Where this comes from
- Record sourced from PubMed, PMID 34726479.
- Also identified by DOI 10.1126/science.abl4784.
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Abstract
The worldwide outbreak of COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global pandemic. Alongside vaccines, antiviral therapeutics are an important part of the healthcare response to countering the ongoing threat presented by COVID-19. Here, we report the discovery and characterization of PF-07321332, an orally bioavailable SARS-CoV-2 main protease inhibitor with in vitro pan-human coronavirus antiviral activity and excellent off-target selectivity and in vivo safety profiles. PF-07321332 has demonstrated oral activity in a mouse-adapted SARS-CoV-2 model and has achieved oral plasma concentrations exceeding the in vitro antiviral cell potency in a phase 1 clinical trial in healthy human participants.
Medical subject headings
- Lactams
- Leucine
- Nitriles
- Proline
- SARS-CoV-2
- Viral Protease Inhibitors
- COVID-19 Drug Treatment