a Department of Molecular and Medical Pharmacology , David Geffen School of Medicine at UCLA , Los Angeles , CA , USA.
b Department of Nuclear Medicine , Ludwig-Maximilians-University of Munich , Munich , Germany.
Expert Rev Mol Diagn. 2016 Nov;16(11):1177-1188. doi: 10.1080/14737159.2016.1243057. Epub 2016 Oct 14.
Prostate specific membrane antigen (PSMA) has become an attractive diagnostic and therapeutic target for small molecule ligands. Radionuclide-chelating ligands can be labeled with either Ga for positron-emission-tomography (PET) or Lu for radionuclide therapy. Areas covered: In this literature review we evaluate the diagnostic value of Ga PSMA PET/CT and the therapeutic potential of Lu PSMA radioligand therapy (RLT) in patients with prostate cancer. Ga PSMA PET/CT is more accurate than CT for nodal staging and superior to conventional imaging in patients with biochemical recurrence, translating into major changes in clinical management. The preliminary data for Lu PSMA indicates >50% reduction of PSA levels in up to 59% of patients. Severe adverse events occurred <10% of patients after RLT. Expert commentary: PSMA ligands for diagnostic and therapeutic purpose will significantly impact the management of patients with prostate cancer.
前列腺特异性膜抗原（PSMA）已成为小分子配体用于诊断和治疗的有吸引力的靶标。放射性核素螯合配体可以用 Ga 进行正电子发射断层扫描（PET），也可以用 Lu 进行放射性核素治疗。涵盖领域：在这篇文献综述中，我们评估了 Ga PSMA PET/CT 的诊断价值，以及 Lu PSMA 放射性配体治疗（RLT）在前列腺癌患者中的治疗潜力。Ga PSMA PET/CT 比 CT 更准确地进行淋巴结分期，并且在生化复发患者中优于传统影像学检查，从而导致临床管理的重大变化。Lu PSMA 的初步数据表明，高达 59%的患者 PSA 水平降低超过 50%。RLT 后，严重不良事件发生率<10%。专家评论：用于诊断和治疗目的的 PSMA 配体将显著影响前列腺癌患者的管理。
