Rahmati Hiva, Mousavi Seyed Mehdi, Souri Zobin, Farzipour Soghra, Tavani Amin Ebrahimi, Jalali-Zefrei Fatemeh
Department of Pharmacology and Toxicology, School of Pharmacy, Guilan University of Medical Sciences, Rasht, Iran.
Department of Cardiology, Cardiovascular Diseases Research Center, Heshmat Hospital, School of Medicine, Guilan University of Medical Sciences, Rasht, Iran.
Anticancer Agents Med Chem. 2025;25(16):1198-1217. doi: 10.2174/0118715206357095250306051714.
Breast cancer (BC) remains a predominant cause of mortality among women, with early diagnosis and ongoing monitoring being crucial for effective management. Integrating nuclear medicine with radiological modalities offers non-invasive anatomical and functional information, enabling precise target localization and quantification. This approach guided the selection of the most appropriate personalized treatment and predicted its efficacy, reducing the use of unnecessary drugs and lowering patient management costs. Since 2020, significant breakthroughs have been made in the development of radiopharmaceuticals, which are different in importantly targeting agents and radionuclides, with a focus on their efficacy in preclinical studies. This review accentuates the central role of radiopharmaceuticals in recent advancements for both imaging and therapeutic applications in BC. We discussed various receptor-targeted radiopharmaceutical therapy (RPT) agents currently utilized in clinical and preclinical settings with their chemical structures, along with the challenges faced in their implementation, including angiotensin II type 1 receptor (AT1 receptor), integrins αvβ3, chemokine receptor (CXCR4), and trophoblast cell-surface antigen-2 (TROP2), cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor, and epithelial cell adhesion molecule (EpCAM)-targeted, epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), fibroblast activation protein inhibitor (FAPI), and mucin 1 (MUC1). While numerous promising RPT agents were still in preclinical stages, this review underscored the potential of tailored radiopharmaceuticals to enhance BC diagnosis and treatment, providing novel avenues for personalized medicine.
乳腺癌（BC）仍是女性死亡的主要原因，早期诊断和持续监测对有效治疗至关重要。将核医学与放射学模式相结合可提供非侵入性的解剖和功能信息，实现精确的靶点定位和定量分析。这种方法指导了最合适的个性化治疗方案的选择，并预测其疗效，减少了不必要药物的使用，降低了患者管理成本。自2020年以来，放射性药物的开发取得了重大突破，其靶向剂和放射性核素存在重要差异，重点在于它们在临床前研究中的疗效。本综述强调了放射性药物在BC成像和治疗应用的最新进展中的核心作用。我们讨论了目前在临床和临床前环境中使用的各种受体靶向放射性药物治疗（RPT）剂及其化学结构，以及它们在实施过程中面临的挑战，包括血管紧张素II 1型受体（AT1受体）、整合素αvβ3、趋化因子受体（CXCR4）、滋养层细胞表面抗原-2（TROP2）、细胞周期蛋白依赖性激酶4和6（CDK4/6）抑制剂，以及靶向上皮细胞粘附分子（EpCAM）、表皮生长因子受体（EGFR）、血管内皮生长因子受体（VEGFR）、成纤维细胞活化蛋白抑制剂（FAPI）和粘蛋白1（MUC1）。虽然许多有前景的RPT剂仍处于临床前阶段，但本综述强调了定制放射性药物在增强BC诊断和治疗方面的潜力，为个性化医疗提供了新途径。
