Human pharmacokinetics of WR-2721☆

Abstract The pharmacokinetic properties of WR2721 were investigated in 13 cancer patients given a 150 mg/M 2 intravenous bolus dose of the drug. An average plasma clearance value of 2.17 L/min was obtained. Very little of the drug or the two metabolites, WR1065 and WR33278, were excreted in urine obtained after the blood collection schedule. Plasma concentrations of WR2721 decreased by 94% within 6 minutes of drug administration. The mean value of 6.44 L obtained for the steady-state volume of distribution indicates that the extravascuhu space occupied by the drug is small. These observations suggest that in human cancer patients, WR2721 is rapidly taken up by tissues and converted to metabolites.