Recent developments in predicting CYP-Independent metabolism


Drug Metab Rev. 2021 May 4:1-69. doi: 10.1080/03602532.2021.1923728. Online ahead of print.

ABSTRACT

As lead optimization efforts have successfully reduced metabolic liabilities due to cytochrome P450 (CYP)- mediated metabolism, there has been an increase in the frequency of involvement of non-CYP enzymes in the metabolism of investigational compounds. Although there have been numerous notable advancements in the characterization of non-CYP enzymes with respect to their localization, reaction mechanisms, species differences and identification of typical substrates, accurate prediction of non-CYP mediated clearance, with a particular emphasis with the difficulties in accounting for any extrahepatic contributions, remains a challenge. The current manuscript comprehensively summarizes the recent advancements in the prediction of drug metabolism and the in vitro to in vitro extrapolation of clearance for substrates of non-CYP drug metabolizing enzymes.

PMID:33941024 | DOI:10.1080/03602532.2021.1923728

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