Metabolite Tales Blog

APRIL 4, 2023

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. Oxidation of adagrasib occurs on the methylpyrrolidine group 4.

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Small Molecule FDA Approval FDA Drugs 52

Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

DECEMBER 13, 2023

The pyrazole in a drug compound developed by LEO as an oral IL-17A protein-protein interaction modulator for the treatment of psoriasis and other inflammatory disorders is susceptible to N -glucuronidation. 22(5):803-11; [link] [10] Glucuronidation and UGT isozymes in bladder: new targets for the treatment of uroepithelial carcinomas?

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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). 2022), JBMR Plus, 6: e10557. ACS Med Chem Lett.

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Drugs Small Molecule FDA Approval Metabolic Stability 52

Metabolite Tales Blog

MARCH 1, 2023

9 The evidence here is that treatment with P450 inhibitors removed the toxic effects seen in the compounds of interest. 2018, 26, 965-972 [link] 4a Pharmaceutics, 2022, 14, 1001 [link] 5 Phys. 11 Figure 11 Pyrazoles – more stable to oxidative cleavage? 2017, 30, 1, 13–37 [link] 2a Drug Metab. 1980, 8, 34-38 [link] 4 J.

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Metabolic Stability Pharmacokinetics Drugs Science 52