Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy
Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy
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DOI：
10.1093/annonc/10.suppl_2.s23
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发表时间：
1999-01-01
影响因子：
50.5
通讯作者：
Valkema, R
中科院分区：
文献类型：
--
作者：
Krenning, EP;de Jong, M;Valkema, R
背景资料：用放射性生长抑素类似物[In-111-DTPA（0）]奥曲肽进行肽受体显像，是一种敏感而特异的技术，可显示体内各种肿瘤上生长抑素受体的存在和丰度。目的：用这种技术可以定位原发性肿瘤和神经内分泌癌以及许多其他癌症类型的转移灶。该技术目前用于评估重复给予高剂量[In-111-DTPA（0）]奥曲肽进行肽受体放射性核素治疗（PRRT）的可能性。In-111发射的俄歇电子和转换电子的组织穿透力分别为0.02-10 μ m和200 - 500 μ m.Patients and methods：在I期试验中，用[In-111-DTPA（0）]奥曲肽治疗了30例大多数神经内分泌进展性肿瘤的终末期患者，最大累积患者剂量约为74 GBq。在长达两年的治疗后，除了少数患者出现血小板计数和淋巴细胞亚群的短暂下降外，没有出现重大的临床副作用。在21名接受累积剂量超过20 GBq的患者中，8名患者的病情稳定，另外6名患者的肿瘤大小缩小。有一种倾向，对更好的结果在患者的肿瘤有较高的积累的radioligand.Conclusions：PRRT是可行的，也与In-111作为放射性核素。根据表达肽受体的肿瘤细胞分布的均匀性和肿瘤的大小，β-发射放射性核素，例如，Y-90，标记DOTA-螯合肽，也是有吸引力的候选人PRRT。最近开始了用[Y-90-DOTA（0），Tyr（3）]奥曲肽的第一个PRRT试验。
Background: Peptide receptor scintigraphy with the radioactive somatostatin analogue, [In-111-DTPA(0)]octreotide, is a sensitive and specific technique to show in vivo the presence and abundance of somatostatin receptors on various tumours.Aim: With this technique primary tumours and metastases of neuroendocrine cancers as well as of many other cancer-types can be localised. This technique is currently used to assess the possibility of peptide receptor radionuclide therapy (PRRT) with repeated administrations of high doses of [In-111-DTPA(0)]octreotide. In-111 emits Auger and conversion electrons having a tissue penetration of 0.02-10 mu m and 200 to 500 mu m, respectively.Patients and methods: Thirty end-stage patients with mostly neuroendocrine progressing tumours were treated with [In-111-DTPA(0)]octreotide, up to a maximal cumulative patient dose of about 74 GBq, in a phase I trial.Results: There were no major clinical side effects after up to two years treatment, except that in a few patients a transient decline in platelets counts and lymphocyte subsets occurred. Promising beneficial effects on clinical symptoms, hormone production and tumour proliferation were found. Of the 21 patients who received a cumulative dose of more than 20 GBq, eight patients showed stabilisation of disease and six other patients a reduction in size of tumours. There is a tendency towards better results in patients whose tumours have a higher accumulation of the radioligand.Conclusions: PRRT is feasible, also with In-111 as radionuclide. Depending on the homogeneity of distribution of tumour cells expressing peptide receptors and the size of the tumour, beta-emitting radionuclides, e.g., Y-90, labelled to DOTA-chelated peptides, are also attractive candidates for PRRT. The first PRRT trials with [Y-90-DOTA(0),Tyr(3)]octreotide started recently.