von Guggenberg Elisabeth, Kolenc Petra, Rottenburger Christof, Mikołajczak Renata, Hubalewska-Dydejczyk Alicja
Department of Nuclear Medicine, Medical University of Innsbruck, 6020 Innsbruck, Austria.
Department of Nuclear Medicine, University Medical Centre Ljubljana, 1000 Ljubljana, Slovenia.
Cancers (Basel). 2021 Nov 18;13(22):5776. doi: 10.3390/cancers13225776.
The cholecystokinin-2 receptor (CCK2R) has been a target of interest for molecular imaging and targeted radionuclide therapy for two decades. However, so far CCK2R targeted imaging and therapy has not been introduced in clinical practice. Within this review the recent radiopharmaceutical development of CCK2R targeting compounds and the ongoing clinical trials are presented. Currently, new gastrin derivatives as well as nonpeptidic substances are being developed to improve the properties for clinical use. A team of specialists from the field of radiopharmacy and nuclear medicine reviewed the available literature and summarized their own experiences in the development and clinical testing of CCK2R targeting radiopharmaceuticals. The recent clinical trials with novel radiolabeled minigastrin analogs demonstrate the potential for both applications, imaging as well as targeted radiotherapy, and reinforce the clinical applicability within a theranostic concept. The intense efforts in optimizing CCK2R targeting radiopharmaceuticals has led to new substances for clinical use, as shown in first imaging studies in patients with advanced medullary thyroid cancer. The first clinical results suggest that the wider clinical implication of CCK2R-targeted radiopharmaceuticals is reasonable.
二十年来，胆囊收缩素-2受体（CCK2R）一直是分子成像和靶向放射性核素治疗的关注靶点。然而，到目前为止，CCK2R靶向成像和治疗尚未应用于临床实践。在这篇综述中，介绍了CCK2R靶向化合物的近期放射性药物研发情况以及正在进行的临床试验。目前，正在研发新的胃泌素衍生物以及非肽类物质，以改善其临床应用性能。一组来自放射性药物和核医学领域的专家对现有文献进行了综述，并总结了他们在CCK2R靶向放射性药物研发和临床试验中的经验。近期使用新型放射性标记的小胃泌素类似物进行的临床试验证明了成像和靶向放射治疗这两种应用的潜力，并强化了在诊疗一体化概念中的临床适用性。在优化CCK2R靶向放射性药物方面所做的大量努力已产生了可用于临床的新物质，晚期甲状腺髓样癌患者的首次成像研究表明了这一点。首批临床结果表明，CCK2R靶向放射性药物具有更广泛的临床应用价值是合理的。
