Neels Oliver C, Kopka Klaus, Liolios Christos, Afshar-Oromieh Ali
Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Bautzner Landstrasse 400, 01328 Dresden, Germany.
Faculty of Chemistry and Food Chemistry, School of Science, Technical University Dresden, Mommsenstrasse 4, 01062 Dresden, Germany.
Cancers (Basel). 2021 Dec 13;13(24):6255. doi: 10.3390/cancers13246255.
PSMA has shown to be a promising target for diagnosis and therapy (theranostics) of prostate cancer. We have reviewed developments in the field of radio- and fluorescence-guided surgery and targeted photodynamic therapy as well as multitargeting PSMA inhibitors also addressing albumin, GRPr and integrin αβ. An overview of the regulatory status of PSMA-targeting radiopharmaceuticals in the USA and Europe is also provided. Technical and quality aspects of PSMA-targeting radiopharmaceuticals are described and new emerging radiolabeling strategies are discussed. Furthermore, insights are given into the production, application and potential of alternatives beyond the commonly used radionuclides for radiolabeling PSMA inhibitors. An additional refinement of radiopharmaceuticals is required in order to further improve dose-limiting factors, such as nephrotoxicity and salivary gland uptake during endoradiotherapy. The improvement of patient treatment achieved by the advantageous combination of radionuclide therapy with alternative therapies is also a special focus of this review.
前列腺特异性膜抗原（PSMA）已被证明是前列腺癌诊断和治疗（诊疗一体化）的一个有前景的靶点。我们综述了放射性和荧光引导手术、靶向光动力疗法以及同时靶向白蛋白、胃泌素释放肽前体（GRPr）和整合素αβ的多靶点PSMA抑制剂领域的进展。还提供了PSMA靶向放射性药物在美国和欧洲的监管状况概述。描述了PSMA靶向放射性药物的技术和质量方面，并讨论了新出现的放射性标记策略。此外，还深入探讨了除常用放射性核素之外用于标记PSMA抑制剂的替代物的生产、应用和潜力。为了进一步改善剂量限制因素，如内放射治疗期间的肾毒性和唾液腺摄取，需要对放射性药物进行额外的改进。放射性核素疗法与替代疗法的优势组合所实现的患者治疗改善也是本综述的一个特别重点。
