生长抑素类似物介导靶向显像及治疗的研究现状和进展

放射性核素标记生长抑素类似物对神经内分泌肿瘤进行靶向诊断和靶向治疗已得到临床广泛认可.大多数生长抑素类似物仅对生长抑素受体2具有较高的亲和力,限制了其在临床中的应用.新一代生长抑素类似物如:1,4,7,10-四氮杂环十二烷-N,N',N",N'"-四乙酸-1-萘丙氨酸-奥曲肽(DOTA-NOC)等,可与更多亚型的生长抑素受体结合且具有更高的亲和力,可由发射不同射线的多种核素标记,已引起广泛重视.该文在介绍常规生长抑素类似物的基础上,着重讨论新的生长抑素类似物、新的螯合剂、新的标记核素及其新的组合,展望生长抑素受体介导肿瘤显像及治疗的前景.

The development of somatostatin analogues mediated tumor targeting and therapy

Radionuclide labelled somatostatin analogues have been widely used in the detection of neuro-endocrine tumors.Till now,most of somatostatin analogues only have high affinity to somatostatin receptor 2(SSTR2),further clinical applications was limitted.A new generation of somatostatin analogues such as 1,4,7,10-tetraazacyclodocecane-N,N',N",N'"-tetaraacetic acid-Nal3-octertide(DOTA-NOC)etc,binding to somatostatin receptors not only SSTR2 but other subtypes has been used mainly in preclinical study.In this review,we discussed these new somatostatin analogues,chelating agent,and their new labelled compounds,these new radionuclide labelled somatostatin analogues may hold great promise for the receptor mediated tumor imaging and treatments.