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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

What are the preclinical characteristics of ISM6331, including its efficacy, safety profile, and drug metabolism and pharmacokinetics (DMPK) properties? The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more.

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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

2013, 41, 508-517 [link] 21 J. 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. 2009, 41, 157-167 [link] 19 Molecules. 2020, 25, 4309 [link] 20 Drug Metab.