Internal medicine

Biotechnology

In vivo

Virus

Disease

Coronavirus disease 2019 (COVID-19)

Infectious disease (medical specialty)

Biology

Pandemic

Outbreak

Viral load

Virology

Chemistry

In vitro

Coronavirus

Antiretroviral therapy

Potency

Protease inhibitor (pharmacology)

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)

Clinical trial

Biochemistry

Medicine

Pharmacology

Science

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.

An oral SARS-CoV-2 M <sup>pro</sup> inhibitor clinical candidate for the treatment of COVID-19

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

An oral SARS-CoV-2 M ^pro inhibitor clinical candidate for the treatment of COVID-19