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90Y/177Lu-DOTATOC: From Preclinical Studies to Application in Humans
Pharmaceutics ( IF 4.9 ) Pub Date : 2021-09-13 , DOI: 10.3390/pharmaceutics13091463
Licia Uccelli 1, 2 , Alessandra Boschi 3 , Corrado Cittanti 1, 2 , Petra Martini 1 , Stefano Panareo 2 , Eugenia Tonini 4 , Alberto Nieri 2 , Luca Urso 2 , Matteo Caracciolo 2 , Luca Lodi 2 , Aldo Carnevale 1, 5 , Melchiore Giganti 1, 5 , Mirco Bartolomei 2
Affiliation  

The PRRT (Peptide Receptor Radionuclide Therapy) is a promising modality treatment for patients with inoperable or metastatic neuroendocrine tumors (NETs). Progression-free survival (PFS) and overall survival (OS) of these patients are favorably comparable with standard therapies. The protagonist in this type of therapy is a somatostatin-modified peptide fragment ([Tyr3] octreotide), equipped with a specific chelating system (DOTA) capable of creating a stable bond with β-emitting radionuclides, such as yttrium-90 and lutetium-177. In this review, covering twenty five years of literature, we describe the characteristics and performances of the two most used therapeutic radiopharmaceuticals for the NETs radio-treatment: [90Y]Y-DOTATOC and [177Lu]Lu-DOTATOC taking this opportunity to retrace the most significant results that have determined their success, promoting them from preclinical studies to application in humans.

中文翻译:


90Y/177Lu-DOTATOC:从临床前研究到人体应用



PRRT(肽受体放射性核素疗法)对于无法手术或转移性神经内分泌肿瘤(NET)患者来说是一种很有前景的治疗方法。这些患者的无进展生存期(PFS)和总生存期(OS)与标准疗法相当。此类疗法的主角是生长抑素修饰的肽片段([Tyr3]奥曲肽),配备有特定的螯合系统(DOTA),能够与β发射放射性核素(例如钇90和镥)形成稳定的键。 177.在这篇综述中,我们回顾了二十五年的文献,描述了两种最常用的 NET 放射治疗放射性药物的特性和性能:[ 90 Y]Y-DOTATOC 和 [ 177 Lu]Lu-DOTATOC 借此机会回顾决定其成功的最重要结果,将其从临床前研究推广到人类应用。
更新日期:2021-09-13
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