首次临床证据表明，使用生长抑素受体拮抗剂进行成像具有可行性。
First clinical evidence that imaging with somatostatin receptor antagonists is feasible.
机构信息
Department of Nuclear Medicine, University Hospital Freiburg, Freiburg, Germany.
出版信息
J Nucl Med. 2011 Sep;52(9):1412-7. doi: 10.2967/jnumed.111.088922. Epub 2011 Aug 18.
UNLABELLED
Preclinical studies have indicated that somatostatin receptor (sst)-expressing tumors demonstrate higher uptake of radiolabeled sst antagonists than of sst agonists. In this study, we evaluated whether imaging with sst antagonists was feasible in patients.
METHODS
Biodistribution and tumor uptake of the sst antagonist (111)In-DOTA-pNO(2)-Phe-c(DCys-Tyr-DTrp-Lys-Thr-Cys)DTyrNH(2) ((111)In-DOTA-BASS) were studied in 5 patients with metastatic thyroid carcinoma or neuroendocrine tumors. Findings were compared with (111)In-pentetreotid ((111)In-DTPA-octreotide) scan.
RESULTS
No adverse effects of (111)In-DOTA-BASS (20 μg) were observed. (111)In-DOTA-BASS detected 25 of 28 lesions, whereas (111)In-DTPA-octreotide detected only 17 of 28 lesions. In the same patient, (111)In-DOTA-BASS showed higher tumor and lower renal uptake than (111)In-DTPA-octreotide (3.5 ± 2.8 percentage injected activity [%IA] vs. 1.0 ± 0.99%IA and 1.5 ± 0.3 %IA vs. 2.3 ± 0.7 %IA) at 4 h after injection.
CONCLUSION
Imaging of neuroendocrine tumors with sst antagonists is clinically feasible. The favorable human biodistribution data suggest that sst antagonists could significantly affect peptide receptor-mediated imaging and therapy.
目的
临床前研究表明，生长抑素受体（sst）表达肿瘤对放射性标记的 sst 拮抗剂的摄取高于 sst 激动剂。本研究旨在评估 sst 拮抗剂在患者中的成像是否可行。
方法
在 5 例转移性甲状腺癌或神经内分泌肿瘤患者中，研究了 sst 拮抗剂（111）In-DOTA-pNO2-Phe-c（DCys-Tyr-DTrp-Lys-Thr-Cys）DTyrNH2（（111）In-DOTA-BASS）的生物分布和肿瘤摄取，并与（111）In-pentetreotide（（111）In-DTPA-octreotide）扫描进行比较。
结果
未观察到（111）In-DOTA-BASS（20μg）的不良反应。（111）In-DOTA-BASS 检测到 28 个病灶中的 25 个，而（111）In-DTPA-octreotide 仅检测到 28 个病灶中的 17 个。在同一患者中，（111）In-DOTA-BASS 在注射后 4 小时显示出比（111）In-DTPA-octreotide 更高的肿瘤摄取和更低的肾脏摄取（3.5±2.8%注射活动[IA]比 1.0±0.99%IA 和 1.5±0.3%IA比 2.3±0.7%IA）。
结论
用 sst 拮抗剂对神经内分泌肿瘤进行成像在临床上是可行的。有利的人体生物分布数据表明，sst 拮抗剂可能会显著影响肽受体介导的成像和治疗。
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