An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

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...

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Vydané v:Science (American Association for the Advancement of Science) Ročník 374; číslo 6575; s. 1586
Hlavní autori: Owen, Dafydd R, Allerton, Charlotte M N, Anderson, Annaliesa S, Aschenbrenner, Lisa, Avery, Melissa, Berritt, Simon, Boras, Britton, Cardin, Rhonda D, Carlo, Anthony, Coffman, Karen J, Dantonio, Alyssa, Di, Li, Eng, Heather, Ferre, RoseAnn, Gajiwala, Ketan S, Gibson, Scott A, Greasley, Samantha E, Hurst, Brett L, Kadar, Eugene P, Kalgutkar, Amit S, Lee, Jack C, Lee, Jisun, Liu, Wei, Mason, Stephen W, Noell, Stephen, Novak, Jonathan J, Obach, R Scott, Ogilvie, Kevin, Patel, Nandini C, Pettersson, Martin, Rai, Devendra K, Reese, Matthew R, Sammons, Matthew F, Sathish, Jean G, Singh, Ravi Shankar P, Steppan, Claire M, Stewart, Al E, Tuttle, Jamison B, Updyke, Lawrence, Verhoest, Patrick R, Wei, Liuqing, Yang, Qingyi, Zhu, Yuao
Médium: Journal Article
Jazyk:English
Vydavateľské údaje: 24.12.2021
ISSN:1095-9203, 1095-9203
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Shrnutí: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.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.
Bibliografia:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:1095-9203
1095-9203
DOI:10.1126/science.abl4784