Metabolism of N,N',N"-triethylenethiophosphoramide by CYP2B1 and CYP2B6 results in the inactivation of both isoforms by two distinct mechanisms.

@article{Harleton2004MetabolismON,
  title={Metabolism of N,N',N"-triethylenethiophosphoramide by CYP2B1 and CYP2B6 results in the inactivation of both isoforms by two distinct mechanisms.},
  author={Erin Harleton and Marie R. Webster and Namandj{\'e} N Bumpus and Ute M. Kent and James Michael Rae and Paul F. Hollenberg},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2004},
  volume={310 3},
  pages={1011-9}
}
The anticancer drug N,N,"N"-triethylenethiophosphoramide (tTEPA) inactivated CYP2B6 and CYP2B1 in the reconstituted system in a time-, concentration-, and NADPH-dependent manner indicative of mechanism-based inactivation. The KI value for the inactivation of CYP2B1 was 38 microM, the kinact was 0.3 min(-1), and the t1/2 value was 2.5 min. Spectral carbon… CONTINUE READING