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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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N-glucuronidation: the human element

Metabolite Tales Blog

The pyrazole in a drug compound developed by LEO as an oral IL-17A protein-protein interaction modulator for the treatment of psoriasis and other inflammatory disorders is susceptible to N -glucuronidation. Paine and Aleksandra Galetin (2014). Drug Metabolism and Disposition 42 (4) 650-664; [link]. [2] Polli, Mary F.