Radiolabeled regulatory peptides for imaging and therapy.
Radiolabeled regulatory peptides for imaging and therapy.
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DOI：
10.1097/med.0b013e32833392ac
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发表时间：
2010-02
期刊：
影响因子：
--
通讯作者：
Smith CJ
中科院分区：
文献类型：
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作者：
Nanda PK;Lane SR;Retzloff LB;Pandey US;Smith CJ
本综述的目的是描述使用放射性标记调节肽来诊断和治疗特定人类癌症的新的创新策略。肽受体靶向放射性核素治疗是一种定点放射治疗方法，专门针对大量表达同源受体亚型的人类癌症。理想情况下，该手术仅针对原发性或转移性疾病，并且是微创的，对正常的附带组织几乎没有辐射损伤。为了使此类治疗策略有效，评估治疗方案的毒性、治疗方案的辐射剂量测定以及放射性药物的生物学特征（包括药物的生物分布和药代动力学）至关重要。通过γ-闪烁扫描进行定点分子成像程序可以解决与肽受体靶向放射性核素治疗相关的许多关键问题，因此有必要描述这种治疗策略的临床益处和风险之间的有效平衡。放射性标记的生物活性肽的设计或化学结构的持续发展可以大大提高这些药物的靶向能力，从而为人类癌症的诊断或治疗创造新的创新策略。
The purpose of the present review is to describe new, innovative strategies of diagnosing and treating specific human cancers using a cadre of radiolabeled regulatory peptides. Peptide receptor-targeted radionuclide therapy is a method of site-directed radiotherapy that specifically targets human cancers expressing a cognate receptor-subtype in very high numbers. Ideally, the procedure targets only the primary or metastatic disease and is minimally invasive, with little radiation damage to normal, collateral tissues. For treatment strategies of this type to be effective, it is critical to evaluate the toxicity of the treatment protocol, the radiation dosimetry of the therapeutic regimen, and the biological profile of the radiopharmaceutical, including biodistribution and pharmacokinetics of the drug. Site-directed molecular imaging procedures via γ-scintigraphy can address many of the critical issues associated with peptide receptor-targeted radionuclide therapy and it is, therefore, necessary to describe the effective balance between the clinical benefits and risks of this treatment strategy. Continued development in the design or chemical structure of radiolabeled, biologically active peptides could do much to improve the targeting ability of these drugs, thereby creating new and innovative strategies for diagnosis or treatment of human cancers.