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. Drug metabolism in drug discovery and development. We hope it was a useful two-parter!
Metabolite Tales Blog
AUGUST 2, 2023
To curb O -glucuronidation at that position, a gem-dimethyl group was incorporated, which not only boosted metabolic stability but also resulted in increased potency of “compound 17” An earlier example of how to manage glucuronidation by steric hindrance is illustrated in “compound 25” in the paper by Zhang et al.,
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Synthetic macrocycles in oncology Pactritinib is a multi-kinase JAK2/FLT3 inhibitor used for the treatment of primary and secondary myelofibrosis, approved by the FDA in 2022. Chen et al.,
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Synthetic macrocycles in oncology Pactritinib is a multi-kinase inhibitor used for the treatment of primary and secondary myelofibrosis and was approved by the FDA in 2022. Chen et al., 39, 1544-1556.
Drug Target Review
SEPTEMBER 20, 2023
Complex challenges such as metabolic stability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. To really benefit from AI, the pharmaceutical industry must be more open to data sharing.
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.
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. Figure 4: Optimisation of an IDO1 inhibitor incorporating installation of a gem-dimethyl group to control glucuronidation of a key hydroxyl group.
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