Sartoris D J, Goodwin D A, Meares C F, DeRiemer L H, Fajardo L F
Invest Radiol. 1984 May-Jun;19(3):221-7.
111In-BLEDTA is a bleomycin-containing radiopharmaceutical that has proven useful as a tumor imaging agent. Whole blood distribution and pharmacokinetic parameters were studied in nine cancer patients, and the results compared with previously reported studies using 57Co-bleomycin. In eight patients studied by bolus intravenous injection, 111In-BLEDTA had a beta half-life (t1/2 beta) of 1.3 hours, a terminal-phase half-life (t1/2) of 11.7 hours, a volume of distribution (Vd gamma) of 57.5L/m2, a total body clearance rate (C1b) of 52.8 ml/min/m2, a renal clearance rate (C1r) of 23.3 ml/min/m2, and a 24-hour urinary excretion of 38.1% total administered dose. 111In-BLEDTA and 57Co-bleomycin have similar C1bs but differing Vds. Polymorphonuclear cell uptake of 111In-BLEDTA may explain its shorter t1/2 beta and t1/2, as well as its lower C1r and 24-hour urinary excretion. While the biologic characteristics of 111In-BLEDTA contribute to a greater background activity than is observed in scans with 57Co-bleomycin, its superior physical properties render it clinically more desirable as a tumor-imaging radiopharmaceutical.
铟-111标记的博来霉素乙二胺四乙酸（111In-BLEDTA）是一种含博来霉素的放射性药物，已被证明可作为肿瘤显像剂。对9例癌症患者进行了全血分布和药代动力学参数研究，并将结果与先前报道的使用钴-57标记博来霉素（57Co-bleomycin）的研究进行比较。在8例通过静脉推注进行研究的患者中，111In-BLEDTA的β半衰期（t1/2β）为1.3小时，终末相半衰期（t1/2）为11.7小时，分布容积（Vdγ）为57.5L/m2，全身清除率（Clb）为52.8ml/min/m2，肾脏清除率（Clr）为23.3ml/min/m2，24小时尿排泄量为给药总量的38.1%。111In-BLEDTA和57Co-bleomycin的Clb相似，但Vd不同。111In-BLEDTA被多形核细胞摄取可能解释了其较短的t1/2β和t1/2，以及较低的Clr和24小时尿排泄量。虽然111In-BLEDTA的生物学特性导致其背景活性比57Co-bleomycin扫描中观察到的更高，但其优越的物理特性使其作为肿瘤显像放射性药物在临床上更具优势。
