创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

放射性核素偶联药物的研究进展及临床应用

Research Progress and Clinical Application of Radionuclide Drug Conjugates

  • 摘要: 恶性肿瘤是世界范围内威胁人类生命健康的头号杀手,临床上90%以上实体瘤的治疗效果仍然不能令人满意,尤其是早期诊断和预后不佳。放射性核素偶联药物(RDCs)是基于放射性核素-靶向配体分子偶联技术开发的一种新兴的肿瘤精准诊疗药物。它利用肿瘤抗原特异性的分子载体递送,引导放射性核素精准靶向肿瘤,进行近距离内放射治疗,在肿瘤早期诊断、分期分型和治疗评估方面具有独特优势。目前,RDCs已成为新型抗肿瘤药物研发的热点方向。通过对生长抑素受体、前列腺特异性膜抗原、CXC族趋化因子受体4、纤维母细胞活化蛋白、人类表皮受体生长因子2和神经降压素受体等热门靶点相关的RDCs研究现状及临床应用予以综述,旨在探讨解决肿瘤诊疗的隐匿性和耐药性等难题,为高效、特异性、生物活性稳定的新型RDCs的研发提供新思路。

     

    Abstract: Malignant tumor is the world's biggest health killer threatening human life. Clinically, more than 90% of solid tumor treatment is still not satisfactory, especially early diagnosis and poor prognosis. Radionuclide drug conjugates are emerging tumor precision drugs developed based on radionuclide-targeting ligand molecular coupling technique. It uses tumor antigen-specific molecular carrier delivery to guide radionuclides to precisely target tumors for brachytherapy, which has unique advantages in early diagnosis, stage classification and treatment evaluation of tumors. At present, radionuclide drug conjugates have become a hot topic in the research and development of new antitumor drugs. In this paper, the current research status and clinical application of radionuclide drug conjugates related to somatostatin receptors, prostate specific membrane antigen, CXC chemokine receptor 4, fibroblast activating protein, human epidermal receptor growth factor 2 and neurotensin receptor are reviewed, aiming to provide new clues for solving drug resistance in tumor diagnosis and treatment, and to provide some new ideas for the research and development of novel RDC drugs with high efficiency, specificity and stable biological activity.

     

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