Metabolite Tales Blog

DECEMBER 13, 2023

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.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59

Metabolite Tales Blog

APRIL 4, 2023

Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolic stability. Insights into drug metabolism by cytochromes P450 from modelling studies of CYP2D6-drug interactions. link] [2] Zhang and Tang, 2018. 2018 Sep;8(5):721-732.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52

Metabolite Tales Blog

MARCH 1, 2023

2018, 26, 965-972 [link] 4a Pharmaceutics, 2022, 14, 1001 [link] 5 Phys. 2018, 61, 5, 2041–205 [link] 9 ACS Chem. 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.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Drugs Science 52