Radioligand therapy (RLT) is a targeted treatment modality that combines a tumour-specific ligand with a therapeutic radionuclide. Once administered, the radiopharmaceutical binds selectively to cancer-associated targets, delivering cytotoxic radiation directly to tumour cells while sparing surrounding tissues. Two RLT agents, [177Lu]Lu-DOTA-TATE (Lutathera®) and [177Lu]Lu-PSMA-617 (Pluvicto®), have received regulatory approval for the treatment of advanced gastroenteropancreatic neuroendocrine tumours and metastatic castration-resistant prostate cancer, respectively. As of July 2025, more than 400 clinical trials are registered, exploring novel molecular targets such as FAP, CAIX, and GRPR, as well as alternative radionuclides and combination regimens in both solid and haematologic malignancies. In this review, we describe the design principles and mechanisms of action of RLT, summarise clinical evidence for approved and emerging radiopharmaceuticals, and discuss current global disparities in access and availability. Finally, we outline the main clinical challenges, including fixed dosing regimens, resistance, toxicity, and variability in patient selection and response assessment. Continued research to optimise radiopharmaceutical design, together with investment in infrastructure, workforce capacity, and international collaboration, will be essential to expand access and realise the full potential of RLT as a leading treatment strategy in modern oncology.
放射性配体疗法是一种靶向治疗模式，通过将肿瘤特异性配体与治疗性放射性核素相结合实现精准治疗。放射性药物经给药后能选择性结合肿瘤相关靶点，将细胞毒性辐射直接递送至肿瘤细胞，同时最大程度保护周围正常组织。目前已有两种放射性配体疗法药物获得监管批准：\[177Lu\]Lu-DOTA-TATE（Lutathera®）用于治疗晚期胃肠胰神经内分泌肿瘤，\[177Lu\]Lu-PSMA-617（Pluvicto®）用于治疗转移性去势抵抗性前列腺癌。截至2025年7月，已有超过400项临床试验注册开展，这些研究正在探索FAP、CAIX、GRPR等新型分子靶点，以及针对实体瘤和血液系统恶性肿瘤的替代性放射性核素与联合治疗方案。本综述系统阐述了放射性配体疗法的设计原理与作用机制，总结了已获批及在研放射性药物的临床证据，并探讨了当前全球范围内该疗法可及性存在的显著差异。最后，我们概述了该领域面临的主要临床挑战，包括固定剂量方案、耐药性问题、毒性反应以及患者选择和疗效评估的异质性。通过持续优化放射性药物设计，并加强基础设施、专业人才建设和国际合作，将对于提升放射性配体疗法的可及性、充分发挥其作为现代肿瘤学重要治疗策略的潜力具有至关重要的意义。
Radioligand Therapy in Cancer Management: A Global Perspective
肿瘤(癌症)患者之家