Budman D R
Don Monti Division of Oncology, Department of Medicine, North Shore University Hospital, New York University School of Medicine, Manhasset, NY 11030, USA.
Semin Oncol. 1996 Dec;23(6 Suppl 13):8-14.
Etoposide phosphate (Etopophos; Bristol-Myers Squibb Company, Princeton, NJ) is a water-soluble prodrug of etoposide that is converted in vivo by endogenous phosphatases to the active drug etoposide. This conversion process is efficient and not saturable in humans at doses between 50 and 1,600 mg/m2. The resultant etoposide demonstrates classic pharmacokinetics, and the etoposide phosphates dose is linearly related to peak levels and the area under the concentration-time curve of etoposide. The absence of noxious solvents and the ability to administer the drug in small volumes over short periods make etoposide a phosphate attractive for conventional- and high-dose clinical programs.
磷酸依托泊苷(商品名:Etopophos;百时美施贵宝公司,新泽西州普林斯顿)是依托泊苷的水溶性前体药物,在体内可被内源性磷酸酶转化为活性药物依托泊苷。在人体中,当剂量在50至1600mg/m²之间时,这种转化过程高效且不饱和。生成的依托泊苷呈现出典型的药代动力学特征,磷酸依托泊苷的剂量与依托泊苷的峰值水平以及浓度-时间曲线下面积呈线性相关。由于不存在有害溶剂,且能够在短时间内以小体积给药,磷酸依托泊苷对于传统剂量和高剂量临床方案而言颇具吸引力。