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 …

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 …

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 …

Global prevalence of SARS-CoV-2 3CL protease mutations associated with nirmatrelvir or ensitrelvir resistance

JD Ip, AWH Chu, WM Chan, RCY Leung… - …, 2023 - thelancet.com
Summary Background Nirmatrelvir-ritonavir (Paxlovid) and ensitrelvir are 3-chymotrypsin-
like cysteine protease (3CL pro) inhibitors which have been approved for the treatment of …

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 …

Resistance to nirmatrelvir due to mutations in the Mpro in the subvariants of SARS-CoV-2 Omicron: Another concern?

S Chatterjee, M Bhattacharya, K Dhama, SS Lee… - … Therapy-Nucleic Acids, 2023 - cell.com
The world has faced 3 years of the COVID-19 pandemic with billions of infections, millions of
deaths, and a massive economic crisis. Since the pandemic began, scientists have started to …

The Substitutions L50F, E166A, and L167F in SARS-CoV-2 3CLpro Are Selected by a Protease Inhibitor In Vitro and Confer Resistance To Nirmatrelvir

D Jochmans, C Liu, K Donckers, A Stoycheva… - MBio, 2023 - Am Soc Microbiol
The SARS-CoV-2 main protease (3CLpro) has an indispensable role in the viral life cycle
and is a therapeutic target for the treatment of COVID-19. The potential of 3CLpro-inhibitors …

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-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 …

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 …