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. Mark Andrews, presentation at the 3rd RSC Anglo-Nordic Medicinal Chemistry Symposium, 13th-16th June 2023. [5] PMID: 9733662. [8]

Small Molecule 59

Small Molecule Metabolic Stability Treatment Drugs 59

Metabolite Tales Blog

MARCH 1, 2023

2018, 26, 965-972 [link] 4a Pharmaceutics, 2022, 14, 1001 [link] 5 Phys. 2023, 13, 1, 92- [link] 8 J. 2018, 61, 5, 2041–205 [link] 9 ACS Chem. 2006 , 34, 145-51 [link] 3 Drug Metab. 1980, 8, 34-38 [link] 4 J. Food Drug Anal. 2000, 2, 195-201 [link] 6 Biochem. 1966 98, 266-277 [link] 7 Metabolites.

Metabolic Stability 52

Metabolic Stability Drugs Pharmacokinetics Science 52

Metabolite Tales Blog

MAY 12, 2023

In 2022, fewer of the 19 newly FDA approved small molecule drugs contained F atoms (adagrasib, lenacapavir, oteseconazole, vonoprazan), but this was followed by 3 more approvals of F-containing drugs in the first quarter of 2023 alone (pirtobrutinib, omaveloxolone, leniolisib). Of these 12 drugs, 9 contain at least one fluorine! Elizabeth A.

Drugs 52

Drugs Small Molecule FDA Approval Metabolic Stability 52