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Metabolism of macrocyclic drugs

Metabolite Tales Blog

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. Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders.

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

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. Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders.

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

3 Metabolism differences at steady state Adagrasib, Mirati’s irreversible KRASG12C inhibitor for treatment of non-small cell lung cancer is mainly metabolised by CYP3A4. Interestingly however, since adagrasib (MRTX849) inhibits CYP3A4 following multiple dosing, its metabolism is subsequently taken over by other CYPs.