Pharmacokinetics of oral O6-benzylguanine and evidence of interaction with oral ketoconazole in the rat

@article{Ewesuedo2000PharmacokineticsOO,
  title={Pharmacokinetics of oral O6-benzylguanine and evidence of interaction with oral ketoconazole in the rat},
  author={Reginald B. Ewesuedo and M. Eileen Dolan},
  journal={Cancer Chemotherapy and Pharmacology},
  year={2000},
  volume={46},
  pages={150-155}
}
Purpose: O6-Benzylguanine (BG) is a modulator of the DNA repair protein, O6-alkylguanine-DNA alkyltransferase (AGT). BG is converted in mice, rats and humans to an equally active, yet longer-lived metabolite, O6-benzyl-8-oxoguanine (8-oxo-BG) by CYP1A2, CYP3A4 and aldehyde oxidase. Since intravenous BG is expected to enter phase I development with orally administered anticancer agents such as temozolomide, procarbazine or SarCNU, we determined the bioavailability of orally administered BG, as… CONTINUE READING

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