Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA(0),D-Phe(1),Tyr(3)]octreotide, a promising somatostatin analogue for radionuclide therapy
Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA(0),D-Phe(1),Tyr(3)]octreotide, a promising somatostatin analogue for radionuclide therapy
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DOI：
10.1007/s002590050064
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发表时间：
1997-04-01
期刊：
影响因子：
--
通讯作者：
Macke, HR
中科院分区：
文献类型：
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作者：
deJong, M;Bakker, WH;Macke, HR
在大鼠中研究了[（111）]In-DOTA（0），D-Phe（1），Tyr（3）]奥曲肽（In-111-DOTATOC）的体外奥曲肽受体结合以及Y-90或In-111标记的DOTATOC的体内代谢，并与[In-111-DTPA（0）]奥曲肽[In-111-DTPAOC]进行了比较。发现In-111-DOTATOC对大鼠大脑皮质微粒体中的奥曲肽受体具有与奥曲肽本身相似的亲和力。注射Y-90或In-111标记的DOTATOC后24小时，表达奥曲肽受体的组织胰腺、垂体、肾上腺和肿瘤中的放射性摄取是注射In-111-DTPAOC后的2-6倍。垂体、胰腺、肾上腺和肿瘤中标记DOTATOC的摄取几乎完全被0.5 mg未标记奥曲肽预处理阻断，表明与奥曲肽受体特异性结合。这些结果强烈表明，Y-90-DOTATOC是一种有前途的放射治疗药物，在111-DOTATOC是奥曲肽受体阳性病变的患者，如大多数神经内分泌肿瘤的诊断的潜在价值。
In vitro octreotide receptor binding of [(111)]In-DOTA(0),D-Phe(1),Tyr(3)] octreotide (In-111-DOTATOC) and the in vivo metabolism of Y-90- or In-111-labelled DOTATOC were investigated in rats in comparison with [In-111-DTPA(0)]octreotide [In-111-DTPAOC). In-111-DOTATOC was found to have an affinity similar to octreotide itself for the octreotide receptor in rat cerebral cortex microsomes. Twenty-four hours after injection of Y-90- or In-111-labelled DOTATOC, uptake of radioactivity in the octreotide receptor-expressing tissues pancreas, pituitary, adrenals and tumour was a factor of 2-6 that after injection of In-111-DTPAOC. Uptake of labelled DOTATOC in pituitary, pancreas, adrenals and tumour was almost completely blocked by pretreatment with 0.5 mg unlabelled octreotide, indicating specific binding to the octreotide receptors. These findings strongly indicate that Y-90-DOTATOC is a promising radiopharmaceutical for radiotherapy and that In-111-DOTATOC is of potential value for diagnosis of patients with octreotide receptor-positive lesions, such as most neuroendocrine tumours.