Results 51 to 60 of about 8,661 (182)

The Remarkable Selectivity of Nirmatrelvir

ACS Pharmacology & Translational Science, 2022
The SARS-CoV-2 main protease is among the most attractive targets for the development of therapeutic interventions for COVID-19. Successful candidate agents will not only possess potent on-target activity versus SARS-CoV-2 Mpro but also minimal polypharmacology versus human cysteine proteases.
Damien Y. Duveau, Craig J. Thomas
openaire   +2 more sources

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Substitutions in SARS-CoV-2 Mpro Selected by Protease Inhibitor Boceprevir Confer Resistance to Nirmatrelvir

Viruses, 2023
Nirmatrelvir, which targets the SARS-CoV-2 main protease (Mpro), is the first-in-line drug for prevention and treatment of severe COVID-19, and additional Mpro inhibitors are in development.
Karen Anbro Gammeltoft, Yuyong Zhou, Line Abildgaard Ryberg, Long V. Pham, Alekxander Binderup, Carlos Rene Duarte Hernandez, Anna Offersgaard, Ulrik Fahnøe, Günther Herbert Johannes Peters, Santseharay Ramirez, Jens Bukh, Judith Margarete Gottwein   +11 more
doaj   +1 more source

A Systematic Review of Nirmatrelvir/Ritonavir and Molnupiravir for the Treatment of Coronavirus Disease 2019 [PDF]

BackgroundTo address the need for treatments for patients with coronavirus disease 2019 (COVID-19), 3 therapies have been given either full approval or Emergency Use Authorization.
Haslam, Alyson, Prasad, Vinay
core   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Paxlovid in Kidney Failure: A Review [PDF]

The COVID-19 virus caused a global pandemic that claimed many lives. Various vaccines and drugs are used for COVID-19 both via intravenous and oral routes.
Ardianty, Nonie, Hasmono, Didik, Suharjono   +2 more
core   +2 more sources

Antivirals Targeting Coronavirus RNA‐Dependent RNA Polymerase and Main Protease: From Mechanisms of Action to Outcomes in COVID‐19 Clinical Trials

Microbial Biotechnology, Volume 19, Issue 4, April 2026.
The target sites of COVID‐19 antivirals discussed in the present opinion paper, namely the RNA dependent RNA polymerase Nsp12 and of the main viral protease Nsp5, are indicated by a red star in the overview of the replication cycle of coronavirus SARS‐CoV‐2.
Harald Brüssow
wiley   +1 more source

Pharmacokinetics and Safety of Single and Multiple Doses of Molnupiravir in Healthy Male Chinese Adults: An Open‐Label, Fixed Sequence, Phase 1 Study

Clinical and Translational Science, Volume 19, Issue 4, April 2026.
ABSTRACT Molnupiravir is an orally administered prodrug of β‐D‐N4‐hydroxycytidine (NHC) that is conditionally approved in China for the treatment of mild to moderate COVID‐19 in nonhospitalized adults at high risk of disease progression. Molnupiravir is rapidly absorbed and hydrolyzed to deliver NHC into systemic circulation.
Jixiang Zhu, Danning Zhang, Zhiping Liu, Bei Yan, Yanqiao Zang, Weiwei Zhao, Fang Sun, Brian M. Maas, Mickie H. Cheng, S. Aubrey Stoch, Haiyan Li   +10 more
wiley   +1 more source

Impact of extended-course oral nirmatrelvir/ritonavir in established Long COVID: a case series

Communications Medicine
Background Prior case series suggest that a 5-day course of oral Paxlovid (nirmatrelvir/ritonavir) benefits some people with Long COVID, within and/or outside of the context of an acute reinfection.
Alison K. Cohen, Toni Wall Jaudon, Eric M. Schurman, Lisa Kava, Julia Moore Vogel, Julia Haas-Godsil, Daniel Lewis, Samantha Crausman, Kate Leslie, Siobhan Christine Bligh, Gillian Lizars, JD Davids, Saniya Sran, Michael Peluso, Lisa McCorkell   +14 more
doaj   +1 more source

A case report of a prolonged decrease in tacrolimus clearance due to co-administration of nirmatrelvir/ritonavir in a lung transplant recipient receiving itraconazole prophylaxis

Journal of Pharmaceutical Health Care and Sciences, 2023
Background Drug-drug interaction management is complex. Nirmatrelvir/ritonavir is a potent cytochrome P450 (CYP) 3A inhibitor and influences pharmacokinetics of co-administered drugs.
Ayumi Tsuzawa, Yoshiki Katada, Keisuke Umemura, Mitsuhiro Sugimoto, Asami Nishikawa, Yu-ki Sato, Yuko Yoshida, Noriaki Kitada, Atsushi Yonezawa, Daisuke Nakajima, Hiroshi Date, Tomohiro Terada   +11 more
doaj   +1 more source