[HTML][HTML] In vitro and in vivo characterization of SARS-CoV-2 strains resistant to nirmatrelvir

M Kiso, Y Furusawa, R Uraki, M Imai… - Nature …, 2023 - nature.com
Nirmatrelvir, an oral antiviral agent that targets a SARS-CoV-2 main protease (3CLpro), is
clinically useful against infection with SARS-CoV-2 including its omicron variants. Since …

[HTML][HTML] In vitro and in vivo characterization of SARS-CoV-2 resistance to ensitrelvir

M Kiso, S Yamayoshi, S Iida, Y Furusawa… - Nature …, 2023 - nature.com
Ensitrelvir, an oral antiviral agent that targets a SARS-CoV-2 main protease (3CLpro or
Nsp5), is clinically useful against SARS-CoV-2 including its omicron variants. Since most …

SARS-CoV-2 3CLpro mutations selected in a VSV-based system confer resistance to nirmatrelvir, ensitrelvir, and GC376

E Heilmann, F Costacurta, SA Moghadasi… - Science translational …, 2022 - science.org
Protease inhibitors are among the most powerful antiviral drugs. Nirmatrelvir is the first
protease inhibitor specifically developed against the SARS-CoV-2 protease 3CLpro that has …

Naturally occurring mutations of SARS-CoV-2 main protease confer drug resistance to nirmatrelvir

Y Hu, EM Lewandowski, H Tan, X Zhang… - ACS central …, 2023 - ACS Publications
The SARS-CoV-2 main protease (Mpro) is the drug target of Pfizer's oral drug nirmatrelvir.
The emergence of SARS-CoV-2 variants with mutations in Mpro raised the alarm of potential …

[HTML][HTML] Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir

S Iketani, H Mohri, B Culbertson, SJ Hong, Y Duan… - Nature, 2023 - nature.com
Nirmatrelvir, an oral antiviral targeting the 3CL protease of SARS-CoV-2, has been
demonstrated to be clinically useful against COVID-19 (refs.,). However, because SARS …

Nirmatrelvir, Molnupiravir, and Remdesivir maintain potent in vitro activity against the SARS-CoV-2 Omicron variant

R Rosales, BL McGovern, ML Rodriguez, DK Rai… - BioRxiv, 2022 - biorxiv.org
Variants of SARS-CoV-2 have become a major public health concern due to increased
transmissibility, and escape from natural immunity, vaccine protection, and monoclonal …

[HTML][HTML] Nirmatrelvir-resistant SARS-CoV-2 is efficiently transmitted in female Syrian hamsters and retains partial susceptibility to treatment

R Abdelnabi, D Jochmans, K Donckers, B Trüeb… - Nature …, 2023 - nature.com
The SARS-CoV-2 main protease (3CLpro) is one of the promising therapeutic targets for the
treatment of COVID-19. Nirmatrelvir is the first 3CLpro inhibitor authorized for treatment of …

Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir

S Ullrich, KB Ekanayake, G Otting, C Nitsche - Bioorganic & Medicinal …, 2022 - Elsevier
The COVID-19 pandemic continues to be a public health threat. Multiple mutations in the
spike protein of emerging variants of SARS-CoV-2 appear to impact on the effectiveness of …

Evolutionary and structural insights about potential SARS-CoV-2 evasion of nirmatrelvir

KS Yang, SZ Leeuwon, S Xu… - Journal of medicinal …, 2022 - ACS Publications
The US FDA approval of PAXLOVID, a combination therapy of nirmatrelvir and ritonavir has
significantly boosted our morale in fighting the COVID-19 pandemic. Nirmatrelvir is an …

Nirmatrelvir-resistant SARS-CoV-2 variants with high fitness in an infectious cell culture system

Y Zhou, KA Gammeltoft, LA Ryberg, LV Pham… - Science …, 2022 - science.org
The oral protease inhibitor nirmatrelvir is of key importance for prevention of severe
coronavirus disease 2019 (COVID-19). To facilitate resistance monitoring, we studied …