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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. Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed. It’s metabolised to 3 main metabolites by CYP3A with potential additional involvement of CYP2C8 and CYP2C19.

Drugs 52
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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. Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed. It’s metabolised to 3 main metabolites by CYP3A with potential additional involvement of CYP2C8 and CYP2C19.

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Welcome to new Director David Hulcoop

The Open Targets Blog

This involves scaling up the process of making a few grams of the compound in the lab to hundreds of tonnes in a factory, in an environmentally-friendly, cost-effective way. Process chemistry is incredibly multidisciplinary: in addition to chemists, you need analytical teams to make sure everything is 99.9%