An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Science
; 374(6575): 1586-1593, 2021 Dec 24.
Article
en En
| MEDLINE
| ID: mdl-34726479
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.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Prolina
/
Inhibidores de Proteasa Viral
/
SARS-CoV-2
/
Tratamiento Farmacológico de COVID-19
/
Lactamas
/
Leucina
/
Nitrilos
Tipo de estudio:
Clinical_trials
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Science
Año:
2021
Tipo del documento:
Article
País de afiliación:
Estados Unidos