UGT Investigation

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  • Published date: January 15, 2020
    • Shirley, New York, United States

Drug-drug interaction (DDI) is a major concern when multiple drugs are co-administrated and interfere the metabolism of one another. In effort to minimize DDI liability, a comprehensive understanding of drug metabolism pathway and interference potency on key enzymes is absolutely crucial. In general, enzymes participating in catalyzing chemical conversions during most drug metabolizing process can be characterized as Phase I enzymes (mainly CYP) and Phase II enzymes (such as glutathione-S-transferases and UGT). Particularly, uridine glucuronyl transferase (UGT) represents one predominant enzyme in Phase II, which is involved in the metabolism pathways of 10% of the top 200 prescribed drugs. Additionally, UGT1A1, one UGT isoform, also plays a part in the glucuronidation of many endogenous products, such as bilirubin, estrogens, and flavonoids. Hence, inhibitory or inducing potentials of certain components might not only cause DDI side effects but also impair normal internal metabolism. Currently, UGT profiles are strongly recommended by regulatory authorities as part of in vitro DDI packages for IND submission. .

Jerry Carter
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