Pharmacokinetics of O6-benzylguanine (NSC637037) and its metabolite, 8-oxo-O6-benzylguanine.

  title={Pharmacokinetics of O6-benzylguanine (NSC637037) and its metabolite, 8-oxo-O6-benzylguanine.},
  author={K Y Tserng and Stephen T. Ingalls and Erik M. Boczko and Timothy Peter Spiro and Xiaolin Li and Susan K. Majka and Stanton L. Gerson and James K. V. Willson and Charles L. Hoppel},
  journal={Journal of clinical pharmacology},
  volume={43 8},
O6-Benzylguanine and its metabolite, 8-oxo-O6-benzylguanine, are equally potent inhibitors of the DNA repair enzyme, O6-alkylguanine-DNA alkyltransferase. Pharmacokinetic values are derived from cancer patients participating in a phase I trial (10 or 20 mg/m2 of O6-benzylguanine in a single bolus dose or 10 to 120 mg/m2 as a 60-min constant infusion). A two-compartment model fits the plasma concentration versus time profile of O6-benzylguanine. O6-Benzylguanine is eliminated rapidly from the… CONTINUE READING