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To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolicstability, 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]
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.
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