Gandhi Noopur, Alaseem Ali M, Deshmukh Rohitas, Patel Artiben, Alsaidan Omar Awad, Fareed Mohammad, Alasiri Glowi, Patel Suhaskumar, Prajapati Bhupendra
Department of Pharmaceutical Chemistry, L. M. College of Pharmacy, Ahmedabad, Gujarat, 380005, India.
Department of Pharmacology, College of Medicine, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 13317, Saudi Arabia.
Med Oncol. 2025 Sep 26;42(11):498. doi: 10.1007/s12032-025-03061-0.
Theranostics represents a transformative advancement in nuclear medicine by integrating molecular imaging and targeted radionuclide therapy within the paradigm of personalized oncology. This review elucidates the historical evolution and contemporary clinical applications of theranostics, emphasizing its pivotal role in precision cancer management. The theranostic approach involves the coupling of diagnostic and therapeutic radionuclides that target identical molecular biomarkers, enabling simultaneous visualization and treatment of malignancies such as neuroendocrine tumors (NETs), prostate cancer, and differentiated thyroid carcinoma. Key theranostic radiopharmaceutical pairs, including Gallium-68-labeled DOTA-Tyr3-octreotate (Ga-68-DOTATATE) with Lutetium-177-labeled DOTA-Tyr3-octreotate (Lu-177-DOTATATE), and Gallium-68-labeled Prostate-Specific Membrane Antigen (Ga-68-PSMA) with Lutetium-177-labeled Prostate-Specific Membrane Antigen (Lu-177-PSMA), exemplify the "see-and-treat" principle central to this modality. This article further explores critical molecular targets such as somatostatin receptor subtype 2, prostate-specific membrane antigen, human epidermal growth factor receptor 2, CD20, and C-X-C chemokine receptor type 4, along with design principles for radiopharmaceuticals that optimize target specificity while minimizing off-target toxicity. Advances in imaging platforms, including positron emission tomography/computed tomography (PET/CT), single-photon emission computed tomography/CT (SPECT/CT), and hybrid positron emission tomography/magnetic resonance imaging (PET/MRI), have been instrumental in accurate dosimetry, therapeutic response assessment, and adaptive treatment planning. Integration of artificial intelligence (AI) and radiomics holds promise for enhanced image segmentation, predictive modeling, and individualized dosimetric planning. The review also addresses regulatory, manufacturing, and economic considerations, including guidelines from the United States Food and Drug Administration (USFDA) and European Medicines Agency (EMA), Good Manufacturing Practice (GMP) standards, and reimbursement frameworks, which collectively influence global adoption of theranostics. In summary, theranostics is poised to become a cornerstone of next-generation oncology, catalyzing a paradigm shift toward biologically driven, real-time personalized cancer care that seamlessly links diagnosis and therapy.
治疗诊断学通过在个性化肿瘤学范式中整合分子成像和靶向放射性核素治疗，代表了核医学的一项变革性进展。本综述阐明了治疗诊断学的历史演变和当代临床应用，强调了其在精准癌症管理中的关键作用。治疗诊断学方法涉及将针对相同分子生物标志物的诊断性和治疗性放射性核素相结合，从而能够同时对神经内分泌肿瘤（NETs）、前列腺癌和分化型甲状腺癌等恶性肿瘤进行可视化和治疗。关键的治疗诊断放射性药物对，包括镓 - 68标记的DOTA - Tyr3 - 奥曲肽（Ga - 68 - DOTATATE）与镥 - 177标记的DOTA - Tyr3 - 奥曲肽（Lu - 177 - DOTATATE），以及镓 - 68标记的前列腺特异性膜抗原（Ga - 68 - PSMA）与镥 - 177标记的前列腺特异性膜抗原（Lu - 177 - PSMA），体现了这种模式核心的“可视化与治疗”原则。本文进一步探讨了关键的分子靶点，如生长抑素受体2亚型、前列腺特异性膜抗原、人表皮生长因子受体2、CD20和C - X - C趋化因子受体4型，以及放射性药物的设计原则，这些原则在优化靶点特异性的同时将非靶点毒性降至最低。成像平台的进展，包括正电子发射断层扫描/计算机断层扫描（PET/CT）、单光子发射计算机断层扫描/CT（SPECT/CT）以及混合正电子发射断层扫描/磁共振成像（PET/MRI），在精确剂量测定、治疗反应评估和适应性治疗计划中发挥了重要作用。人工智能（AI）和放射组学的整合有望增强图像分割、预测建模和个体化剂量规划。该综述还讨论了监管、制造和经济方面的考虑因素，包括美国食品药品监督管理局（USFDA）和欧洲药品管理局（EMA）的指南、良好生产规范（GMP）标准以及报销框架，这些因素共同影响着治疗诊断学在全球的应用。总之，治疗诊断学有望成为下一代肿瘤学的基石，推动向生物驱动的、实时个性化癌症护理的范式转变，这种护理将诊断和治疗无缝连接起来。
