Peptide-based radiopharmaceuticals for targeted tumor therapy.
Peptide-based radiopharmaceuticals for targeted tumor therapy.
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DOI：
10.2174/09298673113209990219
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发表时间：
2013-12
影响因子：
4.1
通讯作者：
C. Dong;Z. Liu;F. Wang
中科院分区：
文献类型：
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作者：
C. Dong;Z. Liu;F. Wang
针对肿瘤靶向肽受体放射性核素治疗（PRRT），设计并优化了一系列放射性标记肽。PRRT的临床前和临床应用已经显示出在肿瘤反应、总生存率和几种肿瘤患者的生活质量方面有希望的结果。（90）Y-DOTA-TOC和（177）Lu-DOTA-TATE是两种最常见的放射性药物，具有症状改善和完整的临床数据。除了生长激素抑制素类似物外，还开发了放射性标记肽来靶向肿瘤中过度表达的相关受体，例如整合素αvβ3、胃泌素释放肽受体（GRPR）、黑皮质素-1受体（MC 1-R）、胆囊收缩素（CCK）受体和胰高血糖素样肽-1受体（GLP-1 R）。已经设计了几种策略来提高PRRT的治疗效果。例如，放射性标记的肽可以通过氨基酸修饰和放射性核素选择来优化。健康的组织保护剂和多周期的程序可以有效地减少PRRT的副作用。此外，可以应用联合治疗，包括PRRT与手术、化疗剂或放射增敏剂的联合，以增加PRRT的有效性。本文综述了近年来肽类放射性药物在肿瘤靶向PRRT中的研究进展。还描述了目前正在进行临床研究的放射性药物。
A series of radiolabeled peptides have been designed and optimized for tumor-targeted peptide receptor radionuclide therapy (PRRT). Pre-clinical and clinical applications of PRRT have shown promising results on tumor response, overall survival, and quality of life in patients with several kinds of tumors. (90)Y-DOTA-TOC and (177)Lu-DOTA-TATE are two of the most common radiopharmaceuticals with symptomatic improvements and complete clinical data. In addition to somatostatin analogs, radiolabeled peptides have been developed to target the relative receptors overexpressed in the tumors, such as integrin αvβ3, gastrin-releasing peptide receptor (GRPR), melanocortin-1 receptor (MC1-R), cholecystokinin (CCK) receptor, and glucagon-like peptide-1 receptor (GLP-1R). Several strategies have been designed to improve the therapeutic efficacy of PRRT. For instance, radiolabeled peptides could be optimized by the amino acid modification and radionuclide selection. Healthy tissue protective agents and multi-cycle procedures could effectively decrease the side effects of PRRT. Furthermore, combination treatments, including PRRT combined with surgery, chemotherapeutic agents, or radiosensitizing agents could be applied to increase the effectiveness of PRRT. In this review, the current progress of peptide-based radiopharmaceuticals for tumor-targeted PRRT was summarized. Radiopharmaceuticals currently under clinical investigation were also described.