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

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.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59