Shaw L M, Turrisi A T, Glover D J, Bonner H S, Norfleet A L, Weiler C, Kligerman M M
Int J Radiat Oncol Biol Phys. 1986 Aug;12(8):1501-4. doi: 10.1016/0360-3016(86)90203-8.
The pharmacokinetic properties of WR-2721 were investigated in 13 cancer patients given a 150 mg/M2 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, WR-1065 and WR-33278, were excreted in urine obtained after the blood collection schedule. Plasma concentrations of WR-2721 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 extravascular space occupied by the drug is small. These observations suggest that in human cancer patients, WR-2721 is rapidly taken up by tissues and converted to metabolites.
在13名癌症患者中，静脉注射150mg/M²推注剂量的WR-2721，对其药代动力学特性进行了研究。获得的平均血浆清除率值为2.17L/分钟。在采血计划后的尿液中，该药物及其两种代谢产物WR-1065和WR-33278排泄极少。给药后6分钟内，WR-2721的血浆浓度下降了94%。稳态分布容积的平均值为6.44L，表明该药物占据的血管外空间较小。这些观察结果表明，在人类癌症患者中，WR-2721被组织迅速摄取并转化为代谢产物。
