Targeting disseminated melanoma with radiolabelled methylene blue - Comparative bio-distribution studies in man and animals
Targeting disseminated melanoma with radiolabelled methylene blue - Comparative bio-distribution studies in man and animals
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DOI：
10.3109/02841869609101650
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发表时间：
1996-01-01
期刊：
影响因子：
3.1
通讯作者：
Spittle, MF
中科院分区：
文献类型：
--
作者：
Link, EM;Costa, DC;Spittle, MF
用Astatine-211 （At-211； α粒子发射器）标记的3,7-（二甲胺）非那唑硫鎓氯[亚甲基蓝（MTB）]靶向放射治疗色素黑色素瘤在动物模型系统中被证明是非常有效的。由于结果证明了将该治疗方法引入临床，因此在患者中使用[I-123]-MTB和[I-131]-MTB进行生物分布研究的目的是确认放射标记的MTB在黑色素瘤病变中摄取的选择性。研究使用平面和SPECT（单光子发射计算机断层扫描）伽玛照相机进行。在男性色素黑素瘤中发现了放射性碘化MTB的稳定摄取，在单次静脉注射后19小时，肿瘤/周围组织和肿瘤/血液的比率为9。放射性碘化MTB分布的时间依赖动力学与在患有黑素瘤的胸腺小鼠中观察到的相似。静脉注射该化合物后2.5 min （T-1/2 biol = 0.58 min）血液放射性降低约90%。它在各个器官中的滞留时间与血液的特征相同或非常相似。肝脏和肾脏对放射性MTB的快速吸收证实了这些器官在排泄化合物方面的重要性：在注射后的第一个24小时内，25-30%的放射性药物随尿液排出。在观察期间，脑部和眼部至少前14小时内没有明显的放射性MTB残留。
Targeted radiotherapy for pigmented melanoma with 3,7-(dimethylamino) phenazathionium chloride [methylene blue (MTB)] labelled with Astatine-211 (At-211; alpha-particle emitter) proved to be very effective in animal model systems. Since the results justified an introduction of the treatment to the clinic, the aim of the bio-distribution studies using [I-123]-MTB and [I-131]-MTB in patients was to confirm selectiveness of radiolabelled MTB uptake in melanoma lesions. The investigations were carried out using planar and SPECT (single photon emission computed tomography) gamma-cameras. A stable uptake of radioiodinated MTB was found in pigmented melanomas in man, with tumour/surrounding tissue and tumour/blood ratios amounting to 9 at 19 h after a single i.v. injection. A time-dependent kinetics of radioiodinated MTB distribution was similar to that observed in human melanoma-bearing athymic mice. Blood radioactivity decreased by about 90% during the first 2.5 min after i.v. injection of the compound (T-1/2 biol = 0.58 min). Its retention time in various organs was either the same or very similar to that characteristic of the blood. A rapid uptake of radioiodinated MTB in the liver and kidneys confirmed the importance of these organs in excreting the compound: 25-30% of the radioactivity administered was expelled with urine over the first 24 h after the injection. There was no obvious retention of radioiodinated MTB in the brain over the observation period and in the eyes for at least the first 14 h.