Paper Picks
Take a look at our favourite publications around biotransformation and metabolism of drugs in Hypha’s “Paper Picks”.
Hypha's Paper Picks
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.
Discover the recommendations made by the IQ Consortium Metabolite Bioanalysis Working Group around best practice in metabolite bioanalysis during drug development.
Find out why more focus should be placed on major metabolites of locally acting drugs such as the unusual gut metabolites of izencitinib.
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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.