Remove 2008 Remove FDA Approval Remove Metabolic Stability
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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. 2008 Mar;153 Suppl 1(Suppl 1):S82-9. We hope it was a useful two-parter!

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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].

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].

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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. Kuo, Nancy E. Kohl, and George D.

Drugs 52
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Obstacles and innovations of macrocyclic drug development

Drug Target Review

Food and Drug Administration (FDA) approved drugs, macrocycles are used to combat a range of diseases, including cancer, viral, fungal and bacterial infections, neurodegenerative and autoimmune diseases. Nature Reviews Drug Discovery , 7(7):608624, 2008. 5 Macrocycles as drugs Despite accounting for just four percent of the U.S.