Abstract:6-Thioguanine (6TG) is poorly absorbed after oral administration. Bolus injections of 6TG result in high peak concentrations with relatively short-lived plasma concentrations. In vitro studies have shown the importance of prolonged exposure to 6TG. Therefore we administered 6TG by infusion at a dose rate of 2 mg/h over 2 h. In three goats we determined the plasma concentration-time curves of 6TG and its riboside (6TGR). A steady state was reached for 6TG and was almost reached for 6TGR within the 2 h of infusi… Show more
“…The mean steady-state TG CSF concentration was 0.5 lM during CIVI, a concentration that is approximately tenfold higher than the in vitro IC 50 values in human lymphoblastic cell lines [2]. The CSF penetration of 18% observed in our study is similar to the estimated 25% penetration previously observed in an animal model [18]. The CSF penetration of TG is comparable to the CSF penetration of MP [3].…”
TG concentrations that are cytotoxic to human leukemia cell lines can be achieved in plasma after a 60 mg/m2 oral dose of TG and in plasma and CSF during CIVI of TG.
“…The mean steady-state TG CSF concentration was 0.5 lM during CIVI, a concentration that is approximately tenfold higher than the in vitro IC 50 values in human lymphoblastic cell lines [2]. The CSF penetration of 18% observed in our study is similar to the estimated 25% penetration previously observed in an animal model [18]. The CSF penetration of TG is comparable to the CSF penetration of MP [3].…”
TG concentrations that are cytotoxic to human leukemia cell lines can be achieved in plasma after a 60 mg/m2 oral dose of TG and in plasma and CSF during CIVI of TG.
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