Addressing metabolic activation as an integral component of drug design.

@article{Doss2006AddressingMA,
  title={Addressing metabolic activation as an integral component of drug design.},
  author={George A. Doss and Thomas A Baillie},
  journal={Drug metabolism reviews},
  year={2006},
  volume={38 4},
  pages={641-9}
}
Formation of reactive intermediates by metabolism of xenobiotics represents a potential liability in drug discovery and development. Although it is difficult, if not impossible, to predict toxicities of drug candidates accurately, it is prudent to try to minimize bioactivation liabilities as early as possible in the stage of drug discovery and lead optimization. Measurement of covalent binding to liver microsomal proteins in the presence and the absence of NADPH, as well as the use of trapping… CONTINUE READING

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