Nasu Y, Saegusa M, Hara M, Ochi J, Akagi T, Obama T, Tsushima T, Yoshimoto J, Ozaki Y, Matsumura Y
Gan To Kagaku Ryoho. 1987 Apr;14(4):1116-21.
Serum and tissue concentrations of bestrabucil (KM 2210), a combined agent of 17-estradiol and Chlorambucil, were examined in patients with urogenital cancers including those of the kidney, bladder, prostate and testis. We administered orally 100mg (50 mg X 2/day of bestrabucil for 3 days), and determined its plasma levels and metabolites. A maximum drug concentration, i.e., 9.25 ng/ml, was noted 3 hours after administration; a constant plasma level of 5 ng/ml was maintained and the concentration of free chlorambucil was low. After single or consecutive oral administration of bestrabucil (100-300 mg), tumor specimens contained significantly large amounts of bestrabucil in comparison with adjacent normal tissue. Selective accumulation of the active component in tumor tissue suggests the clinical usefulness of bestrabucil.
对包括肾癌、膀胱癌、前列腺癌和睾丸癌在内的泌尿生殖系统癌症患者，检测了17-β-雌二醇与苯丁酸氮芥的复合制剂苯丁酸雌二醇（KM 2210）的血清和组织浓度。我们口服给予100mg（苯丁酸雌二醇50mg×2/天，共3天），并测定其血浆水平和代谢产物。给药后3小时观察到最大药物浓度，即9.25ng/ml；维持5ng/ml的恒定血浆水平，游离苯丁酸氮芥的浓度较低。单次或连续口服苯丁酸雌二醇（100 - 300mg）后，与相邻正常组织相比，肿瘤标本中含有大量的苯丁酸雌二醇。活性成分在肿瘤组织中的选择性蓄积提示苯丁酸雌二醇具有临床应用价值。
