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Metabolism of 2022 FDAapprovedsmallmolecule drugs – Part 1 Does CYP3A4 still rule? By Julia Shanu-Wilson It won’t come as much surprise to learn that of the 17 smallmolecules* approved by the FDA in 2022, CYP3A4 was the major player in drug metabolism. References Iversen et al.,
Metabolism of 2022 FDAapprovedsmallmolecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the smallmolecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. 2008 Mar;153 Suppl 1(Suppl 1):S82-9. Br J Pharmacol.
If successful, this work could result in the repurposing of several FDA-approved therapeutics for the purpose of extending the human lifespan, at a lower cost and over faster timelines than conceivably possible with de novo drug discovery. The Scheibye-Knudsen lab has analyzed 1.5 billion prescriptions from 4.8
In 2021, almost one third of FDAapproved drugs contained at least one fluorine. Even newer from the pharma benches are 12 smallmolecule drugs highlighted by Chris de Savi [4], whose structures were first disclosed at the ACS and AACR meetings in Q1 2023. Of these 12 drugs, 9 contain at least one fluorine! Kuo, Nancy E.
Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 2 Typically, small-molecule drugs target active sites buried inside proteins. What are macrocycles and why are they interesting for drug discovery?
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