Heck M M, Retz M, Tauber R, Knorr K, Kratochwil C, Eiber M
Klinik und Poliklinik für Urologie, Klinikum rechts der Isar, Technische Universität München, Ismaninger Straße 22, 81675, München, Deutschland.
Institut für Nuklearmedizin, Klinikum rechts der Isar, Technische Universität München, Ismaninger Straße 22, 81675, München, Deutschland.
Urologe A. 2017 Jan;56(1):32-39. doi: 10.1007/s00120-016-0274-3.
Radioligand therapy (RLT) directed against prostate-specific membrane antigen (PSMA) enables tumor-specific treatment directed against PSMA-overexpressing prostate cancer cells. Several PSMA ligands such as PSMA-617 or PSMA-I&T have been developed that can be labeled with β‑radiating lutetium-177. These are currently applied in compassionate use programs to treat metastatic castration-resistant prostate cancer (mCRPC). PSMA-directed RLT is currently being offered in several nuclear medicine departments throughout Germany. Several retrospective case series demonstrate its activity with a prostate-specific antigen (PSA) decrease >50% in 30-60% of mCRPC patients. The toxicity seems to be low. Hematologic grade 4 toxicity has not been observed and grade 3 toxicities rarely occur. The main nonhematologic adverse events are intermittent dry mouth because of unspecific PSMA expression in the salivary glands as well as fatigue and nausea. Currently there are no prospective studies available for evaluation of PSMA-targeted RLT and a survival benefit over approved standard therapies such as abiraterone, enzalutamide, radium-223-dichloride, docetaxel or cabazitaxel has not been shown. PSMA-targeted RLT should therefore currently only be offered after critical evaluation in patients who exhausted the approved standard therapies.
针对前列腺特异性膜抗原(PSMA)的放射性配体疗法(RLT)能够对过表达PSMA的前列腺癌细胞进行肿瘤特异性治疗。已经开发出几种PSMA配体,如PSMA-617或PSMA-I&T,它们可以用发射β射线的镥-177进行标记。目前,这些配体正在用于同情用药计划,以治疗转移性去势抵抗性前列腺癌(mCRPC)。德国多个核医学科室目前都在提供PSMA导向的RLT。几个回顾性病例系列证明了其有效性,30%-60%的mCRPC患者前列腺特异性抗原(PSA)下降超过50%。其毒性似乎较低。尚未观察到4级血液学毒性,3级毒性也很少发生。主要的非血液学不良事件是由于唾液腺中PSMA非特异性表达导致的间歇性口干,以及疲劳和恶心。目前尚无前瞻性研究可用于评估PSMA靶向RLT,也未显示其相对于批准的标准疗法(如阿比特龙、恩杂鲁胺、二氯化镭-223、多西他赛或卡巴他赛)具有生存获益。因此,目前仅应在对用尽批准标准疗法的患者进行严格评估后,才提供PSMA靶向RLT。