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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Drug metabolism in drug discovery and development. We hope it was a useful two-parter!

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N-glucuronidation: the human element

Metabolite Tales Blog

To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolic stability, but also resulted in increased potency of the final lead compound. 8(2):3640-3648; [link] [11] Pharmacokinetics of the Multi-kinase Inhibitor Pexidartinib: Mass Balance and Dose Proportionality. Oncotarget.

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Metabolism of five membered nitrogen containing heterocycles

Metabolite Tales Blog

2018, 26, 965-972 [link] 4a Pharmaceutics, 2022, 14, 1001 [link] 5 Phys. 2010, 75, 9, 3141–3143 [link] 22 Clin Pharmacokinet. 44, 797–814 [link] Take a look at our other blogs The post Metabolism of five membered nitrogen containing heterocycles appeared first on Hypha Discovery. 2017, 30, 1, 13–37 [link] 2a Drug Metab.