Remove 2013 Remove Disease Remove Metabolic Stability
article thumbnail

Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more. The novel molecules were further ranked based on their ADME and selectivity profiles.

article thumbnail

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]. 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.

Drugs 52
Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

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]. 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.

article thumbnail

N-glucuronidation: the human element

Metabolite Tales Blog

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. Figure 4: Optimisation of an IDO1 inhibitor incorporating installation of a gem-dimethyl group to control glucuronidation of a key hydroxyl group.

article thumbnail

Obstacles and innovations of macrocyclic drug development

Drug Target Review

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.