Paper Picks
Take a look at our favourite publications around biotransformation and metabolism of drugs in Hypha’s “Paper Picks”.
Hypha's Paper Picks
An interesting paper on oxidative biotransformation of elinzanetant by CYP3A4 to 3 active metabolites is the subject of our paper pick for February 2025.
In this paper an IQ Consortium industry working group provide interesting insights into in vitro MetID practices and their effectiveness in predicting circulating human metabolites.
Major biotransformation routes of aficamten involving hydroxylation, onwards glucuronidation and gut metabolism are highlighted and discussed in this article.
There are several interesting facets to this paper in which the ADME characteristics and major circulating glucuronides of icenticaftor are discussed.
Two recent papers exploring the role of NMR spectroscopy in drug discovery and development have prompted us to highlight the role of NMR in drug metabolism in our blog this month.
The discovery of novel human metabolites of inavolisib derived from the heme breakdown product stercobilin is the topic of our paper pick this month.
Our paper pick for July 2024 highlights the the first-ever identification of an aldehyde oxidase-mediated DDI involving OSI-930 and inhibition of AO metabolism by erlotinib.
This paper highlights how a single biotransformation event led to several unusual metabolites that were proposed to arise from intramolecular reactions and chemical degradation of a key reactive metabolite.
Our paper pick for April 2024 discusses the reasons and strategies for replacing a carboxylic acid with a bioisostere. Of particular interest is the use of structural biology to identify neutral bioisosteres that rely on less commonly explored cation π-interactions.
Our highlighted paper for March 2024 looks at how chemists investigated and overcame anticoagulation mediated toxicity caused by an aldehyde oxidase metabolite.
Our choice for February comprises two papers looking at the impact of metabolism-mediated loss of radiolabel in human mass balance studies.
Our first paper pick for 2024 describes the discovery of IRAK4 inhibitors which benefited from inclusion of 2 hydroxyl groups at different positions in the structures.
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.