Cytochrome P450 Mediated Bioactivation of Saracatinib.

  title={Cytochrome P450 Mediated Bioactivation of Saracatinib.},
  author={Jiaming Chen and Y. N. Peng and Jiang Zheng},
  journal={Chemical research in toxicology},
  volume={29 11},
Saracatinib is a highly selective Src kinase inhibitor against all Src kinase family members and has demonstrated anticancer effects in preclinical models. Unfortunately, it has shown multiple adverse effects during its clinical trials, along with time-dependent inhibition of P450 enzymes. The major objective of this study was to identify reactive metabolites of saracatinib in vitro and in vivo. Four oxidative metabolites (M1-M4) were detected in rat and human liver microsomal incubation… CONTINUE READING
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