Prostate cancer remains one of the most common malignancies in men worldwide, with incidence and mortality steadily increasing across diverse populations. While early detection and radical prostatectomy can achieve durable control in a subset of patients, approximately 40% of men will ultimately experience biochemical recurrence often in the absence of clinically detectable disease. Conventional imaging approaches—CT, MRI, and bone scintigraphy—have limited sensitivity for early relapses, frequently leading to delayed diagnosis and suboptimal treatment planning. The discovery of prostate-specific membrane antigen (PSMA) in 1987 and its subsequent clinical translation into positron emission tomography (PET) imaging with [68Ga]Ga-PSMA-11 in 2012, followed by U.S. FDA approval in 2020, has transformed the landscape of prostate cancer imaging. PSMA PET has demonstrated superior accuracy over conventional imaging, as highlighted in the landmark proPSMA trial and now serves as the foundation for theranostic approaches that integrate diagnostic imaging with targeted radioligand therapy. The clinical approval of [177Lu]Lu-PSMA-617 (Pluvicto®: (lutetium Lu 177 vipivotide tetraxetan, Advanced Accelerator Applications USA, Inc., a Novartis company) has established targeted radioligand therapy as a viable option for men with metastatic castration-resistant prostate cancer, extending survival in patients with limited alternatives. Emerging strategies, including next-generation ligands with improved tumor uptake and altered clearance pathways, as well as the integration of artificial intelligence for imaging quantification, are poised to further refine patient selection, dosimetry, and treatment outcomes. This review highlights the evolution of PSMA-based imaging and therapy, discusses current clinical applications and limitations, and outlines future directions for optimizing theranostic strategies in prostate cancer care.
前列腺癌仍是全球男性最常见的恶性肿瘤之一，在不同人群中发病率和死亡率持续上升。虽然早期检测和根治性前列腺切除术可使部分患者获得长期控制，但约40%的患者最终会出现生化复发，且通常无临床可检测的疾病表现。传统影像学方法（CT、MRI和骨显像）对早期复发的敏感性有限，常导致诊断延迟和治疗方案欠佳。前列腺特异性膜抗原（PSMA）于1987年被发现，随后在2012年临床转化为[⁶⁸Ga]Ga-PSMA-11正电子发射断层扫描（PET）成像，并于2020年获得美国FDA批准，彻底改变了前列腺癌影像学格局。PSMA PET已证明其准确性优于传统影像学，这在具有里程碑意义的proPSMA试验中得到印证，并成为融合诊断影像与靶向放射性配体疗法的诊疗一体化策略的基础。[¹⁷⁷Lu]Lu-PSMA-617（Pluvicto®：镥[¹⁷⁷Lu]维帕妥肽注射液，诺华旗下美国先进加速器应用公司）的临床批准，使靶向放射性配体疗法成为转移性去势抵抗性前列腺癌患者的可行选择，为治疗选择有限的患者延长了生存期。新兴策略包括具有更高肿瘤摄取和改良清除途径的新一代配体，以及结合人工智能进行影像量化分析，有望进一步优化患者选择、剂量测定和治疗效果。本综述重点阐述PSMA靶向诊疗技术的发展历程，讨论当前临床应用与局限，并展望优化前列腺癌诊疗一体化策略的未来方向。
肿瘤(癌症)患者之家