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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

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. Adagrasib metabolism after single and multiple oral dosing in humans.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Metabolism of de novo-designed macrocyclic drugs approved by the FDA By Julia Shanu-Wilson To date, only 4% (67) of FDA approved drugs are macrocycles [1]. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Balazs et al.,

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Metabolism of de novo-designed macrocyclic drugs approved by the FDA By Julia Shanu-Wilson To date, only 4% (67) of FDA approved drugs are macrocycles [1]. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Balazs et al.,

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Breaking C-F bonds in drugs

Metabolite Tales Blog

In 2021, almost one third of FDA approved drugs contained at least one fluorine. This was surprising given that replacement of a phenyl with a pyrimidine and fluorination of aryl or heteroaryl rings are techniques often used to increase metabolic stability. 3] The Fluorination of C-H Bonds: Developments and Perspectives.

Drugs 52