Metabolite Tales Blog

JULY 5, 2023

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]. However, in the quest to tackle challenging disease targets with difficult drug binding sites, there is revived interest in developing this compound type to offer unique solutions.

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Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

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]. However, in the quest to tackle challenging disease targets with difficult drug binding sites, there is revived interest in developing this compound type to offer unique solutions.

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

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. Paine and Aleksandra Galetin (2014). Drug Metabolism and Disposition 42 (4) 650-664; [link]. [2] Polli, Mary F.

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Small Molecule Metabolic Stability Treatment Drugs 59

Drug Target Review

JANUARY 16, 2025

These sites are commonly involved in protein-protein interactions, some of which are key to disease development. 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.

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Drug Development Small Molecule Drugs FDA Approval 52