An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Science
; 374(6575): 1586-1593, 2021 Dec 24.
Article
in English
| MEDLINE | ID: covidwho-1666355
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.
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Proline
/
Viral Protease Inhibitors
/
SARS-CoV-2
/
COVID-19 Drug Treatment
/
Lactams
/
Leucine
/
Nitriles
Type of study:
Prognostic study
/
Randomized controlled trials
Topics:
Vaccines
Limits:
Animals
/
Humans
Language:
English
Journal:
Science
Year:
2021
Document Type:
Article
Affiliation country:
Science.abl4784
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