Metabolite Tales Blog
Hypha’s “Metabolite Tales” blog articles are purely science-focussed commentary on interesting developments and papers relevant to the role of metabolism in drug discovery and development. The content is particularly relevant to those with a background in medicinal chemistry, drug metabolism and biotransformation.
We also recommend the following excellent blogs:
Drug Hunter – a trusted, independent source of curated, factual information for the drug discovery community, in particular the articles, case studies and cheat sheets!
In The Pipeline – Derek Lowe’s commentary on drug discovery and the pharma industry.
Hypha's Metabolite Tales Blog Articles
In this blog we look at motifs and scaffolds of F-containing drugs that are subject to metabolism mediated defluorination, along with some drug design strategies that have been used to circumvent this.
In this follow-up blog, we dig into the drugs approved by the FDA in 2022 that are cleared by multiple CYPs, mixed phase mechanisms and through involvement of gut metabolism.
Our blog this month highlights trends in metabolism of five membered nitrogen containing aromatic heterocycles in drug compounds.
In Part 1 of this blog on metabolism of small molecules approved by the FDA in 2022 we look at the trends, and whether CYP3A4 still rules.
Andrew Parkinson, Consultant and former Founder and CSO/CEO at Xenotech, debates whether drugs that induce CYP1A enzymes via activation of the AhR receptor should be a cause for concern or not.
In this blog we look at metabolism of covalent drugs, highlighting some interesting stories from the field and metabolism quirks of covalent inhibitors.
The majority of reviews on the application of bioisosteres are focused on effects on potency. In this blog we focus on how bioisosteres can alter metabolism of a drug.
Here we discuss metabolism of drugs in which CYPs catalyse oxidation of tert-butyl groups.
This blog highlights the prospect of exploiting orphan human CYPs for development of targeted anti-cancer agents through a prodrug strategy.
In this blog Consultant and Medicinal Chemistry expert Rob Young explores some of the potential impacts of hydroxyl groups in medicinal chemistry, contextualising opportunities alongside other fundamental structural changes and considering the physical consequences of its introduction.
Steve Djuric, Consultant and ex VP of Medicinal Chemistry at Abbvie, shares his thoughts on the challenges we face today in selecting drug candidates.
In this blog Steve delves into some of the PK demands, including permeability of PROTACs, CYP and AO metabolism, and the impact of AI.
Our guest blogger Guy Webber discusses the reasons for de-risking DMPK and why he advises integrating metabolic de-risking into drug discovery processes.
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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.