Wafelman A R, Hoefnagel C A, Maessen H J, Maes R A, Beijnen J H
Department of Pharmacy, Slotervaart Hospital, Amsterdam, The Netherlands.
Eur J Nucl Med. 1997 May;24(5):544-52. doi: 10.1007/BF01267687.
Iodine-131 labelled meta-iodobenzylguanidine ([131I]MIBG) is used for diagnostic scintigraphy and radionuclide therapy of neural crest-derived tumours. After administration of therapeutic doses of [131I]MIBG (3.1-7.5 GBq) to 17 patients (n=32 courses), aged 2-73 years, 56%+/-10%, 73%+/-11%, 80%+/-10% and 83%+/-10% of the dose was cumulatively excreted as total radioactivity in urine at t=24 h, 48 h, 72 h and 96 h, respectively. Except for two adult patients, who showed excretion of 14%-18% of [131I]meta-iodohippuric acid ([131I]MIHA), the cumulatively excreted radioactivity consisted of >85% [131I]MIBG, with 6% of the dose excreted as free [131I]iodide, 4% as [131I]MIHA and 2.5% as an unknown iodine-131 labelled metabolite. Cumulative renal excretion rates of total radioactivity and of [131I]MIBG appeared to be higher in neuroblastoma and phaeochromocytoma patients than in carcinoid patients. Based on the excretion of small amounts of [131I]meta-iodobenzoic acid in two patients, a possible metabolic pathway for [131I]MIBG is suggested. The degree of metabolism was not related to the extent of liver uptake of radioactivity.
碘 - 131标记的间碘苄胍([131I]MIBG)用于神经嵴源性肿瘤的诊断性闪烁显像和放射性核素治疗。对17例年龄在2至73岁的患者(n = 32个疗程)给予治疗剂量的[131I]MIBG(3.1 - 7.5 GBq)后,在t = 24小时、48小时、72小时和96小时时,分别有56%±10%、73%±11%、80%±10%和83%±10%的剂量以总放射性形式累积排泄到尿液中。除了两名成年患者排泄出14% - 18%的[131I]间碘马尿酸([131I]MIHA)外,累积排泄的放射性中>85%为[131I]MIBG,其中6%的剂量以游离[131I]碘化物形式排泄,4%以[131I]MIHA形式排泄,2.5%以一种未知的碘 - 131标记代谢物形式排泄。神经母细胞瘤和嗜铬细胞瘤患者中总放射性和[131I]MIBG的累积肾排泄率似乎高于类癌患者。基于两名患者中少量[131I]间碘苯甲酸的排泄情况,提出了[131I]MIBG可能的代谢途径。代谢程度与肝脏放射性摄取程度无关。