A novel strategy for ADME screening of prodrugs: combined use of serum and hepatocytes to integrate bioactivation and clearance, and predict exposure to both active and prodrug to the systemic circulation.

@article{Hoppe2014ANS,
  title={A novel strategy for ADME screening of prodrugs: combined use of serum and hepatocytes to integrate bioactivation and clearance, and predict exposure to both active and prodrug to the systemic circulation.},
  author={Edmund Hoppe and N J Hewitt and Hans-Peter Buchstaller and Hans-Michael Eggenweiler and Christian Sirrenberg and Astrid Zimmermann and Joachim M{\"a}rz and Harold L. Schwartz and Christoph Saal and Michael Meyring and Stefan Hecht},
  journal={Journal of pharmaceutical sciences},
  year={2014},
  volume={103 5},
  pages={
          1504-14
        }
}
Common strategies to optimize prodrugs use either in vitro or rodent in vivo approaches, which do not consider elimination pathways that do not result in the generation of the desired product or might be misleading because of species differences, respectively. As a step forward, we have incorporated a novel application of hepatocytes into our prodrug optimization strategy to increase the bioavailability of a poorly soluble drug candidate by attaching a charged ester linker. The model involves… CONTINUE READING
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