Results 31 to 40 of about 6,478 (160)

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

Development of a physiologically‐based pharmacokinetic model for Ritonavir characterizing exposure and drug interaction potential at both acute and steady‐state conditions

CPT: Pharmacometrics &Systems Pharmacology, Volume 14, Issue 3, Page 523-539, March 2025.
Abstract Ritonavir (RTV) is a potent CYP3A inhibitor that is widely used as a pharmacokinetic (PK) enhancer to increase exposure to select protease inhibitors. However, as a strong and complex perpetrator of CYP3A interactions, RTV can also enhance the exposure of other co‐administered CYP3A substrates, potentially causing toxicity.
Lien Thi Ngo, Woojin Jung, Tham Thi Bui, Hwi‐yeol Yun, Jung‐woo Chae, Jeremiah D. Momper   +5 more
wiley   +1 more source

The Impact of Common Medications on Male Fertility: An Updated Systematic Review

Andrology, EarlyView.
ABSTRACT Background Compared with those of cytotoxic treatments, the potential effects of common medications on the fertility of men trying to conceive currently or planning to conceive in the future are less well described. The use of common medications may modify the gonadotropic axis, spermatogenesis, and epididymal maturation or alter male ...
Lina Jebli, Salomé Gallissian, Roxanne Barèges, Félicia Fournier, Catherine Metzler‐Guillemain, Ségolène Prades, Fanny Magnan‐Sebag, Jeanne Perrin   +7 more
wiley   +1 more source

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

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

Tacrolimus Toxicity in Two Renal Transplant Recipients Treated With Nirmatrelvir/Ritonavir: A Case Series

Annals of Internal Medicine: Clinical Cases, 2023
Since the onset of the SARS-CoV-2 (COVID-19) pandemic, significant effort has been devoted toward developing therapeutics that decrease the morbidity and mortality of COVID-19 infection.
Meaghan Coyne, Myint Aye
doaj   +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

Prevalence of potentially inappropriate use of antiviral therapy with simnotrelvir-ritonavir versus nirmatrelvir-ritonavir in hospitalised patients: a retrospective study in Beijing, China

BMJ Open Respiratory Research
Background While simnotrelvir-ritonavir and nirmatrelvir-ritonavir, the oral antiviral agents targeting the 3C-like proteases, are widely used in China, robust data on their appropriate use remain limited in hospitalised patients.
Hui Zhang, Hui Yang, Yi Zhang, Jia Li, Han Wu, Xintong Zhang, Zhuoling An, Yuezhen Zhu, Chunguo Jiang, Wanying Chen   +9 more
doaj   +1 more source

Thermodynamic characterisation of covalent ligand binding

British Journal of Pharmacology, EarlyView.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman, Maayan Lavie, Almog Nadir, Ronen Gabizon, Nir London   +4 more
wiley   +1 more source

Emerging small-molecule antiviral agents in long COVID prevention

Frontiers in Pharmacology
Long COVID, or Post-Acute Sequelae of COVID-19 (PASC), was characterized by persistent symptoms such as fatigue, shortness of breath, and cognitive impairments.
Xiaomeng He, Xiang Zhang, Wu Zhong
doaj   +1 more source