Arsenault Frédéric, Beauregard Jean-Mathieu, Pouliot Frédéric
Department of Radiology and Nuclear Medicine and Cancer Research Center.
Division of Nuclear Medicine, Department of Medical Imaging and Oncology Branch of Research Center, CHU de Québec.
Curr Opin Support Palliat Care. 2018 Sep;12(3):359-365. doi: 10.1097/SPC.0000000000000357.
In recent years, major advances in molecular imaging of prostate cancers (PCa) were made with the development and clinical validation of highly accurate PET tracers to stage and restage the disease. Prostate-specific membrane antigen (PSMA) is a transmembrane protein highly expressed in PCa, and its expression has led to the development of PSMA-binding radiopharmaceuticals for molecular imaging or radioligand therapy (RLT). We herein review the recent literature published on diagnostic and therapeutic (i.e. theranostic) PSMA tracers.
Development in small PSMA-targeted molecules labeled with gallium-68 and fluorine-18 show promising results for primary staging and detection of disease at biochemical recurrence using PET/computed tomography (PET/CT). Studies show a higher sensitivity and specificity, along with an improved detection rate over conventional imaging (CT scan and bone scan) or choline PET tracers, especially for restaging after prostate-specific antigen failure following loco-regional therapy. In addition, some PSMA tracers can be labeled with beta-minus and alpha particle emitters, yielding encouraging response rates and low toxicity, and potentially offering a new line of targeted therapy for metastatic castration-resistant PCa.
PSMA-targeted tracers have shown unprecedented accuracy to stage and restage PCa using PET/CT. Given their specific biodistribution toward PCa tissue, PSMA RLT now offers new therapeutic possibilities to target metastatic PCa. Prospective multicenter randomized studies investigating the clinical impact of PSMA-targeted molecules are urgently needed.
近年来，随着高精度PET示踪剂的开发和临床验证，前列腺癌（PCa）分子成像取得了重大进展，可用于疾病分期和再分期。前列腺特异性膜抗原（PSMA）是一种在PCa中高度表达的跨膜蛋白，其表达促使开发了用于分子成像或放射性配体治疗（RLT）的PSMA结合放射性药物。我们在此综述了最近发表的关于诊断和治疗（即诊疗一体化）PSMA示踪剂的文献。
用镓-68和氟-18标记的小分子PSMA靶向分子的开发，在使用PET/计算机断层扫描（PET/CT）对疾病进行初次分期和生化复发检测方面显示出有前景的结果。研究表明，与传统成像（CT扫描和骨扫描）或胆碱PET示踪剂相比，其具有更高的敏感性和特异性，以及更高的检测率，特别是在局部区域治疗后前列腺特异性抗原失败后的再分期方面。此外，一些PSMA示踪剂可以用β-和α粒子发射体标记，产生令人鼓舞的缓解率和低毒性，并可能为转移性去势抵抗性PCa提供新的靶向治疗方法。
PSMA靶向示踪剂在使用PET/CT对PCa进行分期和再分期方面显示出前所未有的准确性。鉴于其对PCa组织的特异性生物分布，PSMA RLT现在为靶向转移性PCa提供了新的治疗可能性。迫切需要进行前瞻性多中心随机研究，以调查PSMA靶向分子的临床影响。
