How MetID studies can improve safety and efficacy in PROTAC drugs 

[Image courtesy of Wuxi AppTec]

Most drugs undergo some degree of biotransformation after being administered. This metabolism process allows a drug’s active pharmaceutical ingredient (API) to achieve its desired effect or be eliminated. Metabolism also creates innumerable metabolites that can stimulate or inhibit enzymes, cultivate a chemical reaction or defend against other organisms in vivo. For these reasons, metabolites that exceed 10% of total exposures to drug-related components in humans must be identified and characterized through targeted toxicological studies called metabolite identification (“MetID”) studies.

In vitro MetID assays are simple, rapid and can achieve high throughput. They can also be used to predict in vivo metabolism, thereby saving experimental test species. In vivo, MetID studies on animal bile, urine and feces can provide information on the drug’s metabolic an…

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