State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Stability of Biopharmaceuticals, Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.
State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Stability of Biopharmaceuticals, Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.
Drug Discov Today. 2019 Oct;24(10):2096-2104. doi: 10.1016/j.drudis.2019.06.011. Epub 2019 Jun 19.
Low-molecular-weight heparin (LMWH) has attracted increasing attention as a tumor treatment because of its board range of physiological functions. Over the past decade, diverse LMWH derivatives have increased the variety of antitumor strategies available, serving not only as anti-tumor agents, but also as drug delivery platforms. In this review, we introduce the basic strategy for structural modification of LMWH to attenuate its antitumor activity while reducing its risk of bleeding and immune responses, as well as highlighting current applications of LMWH and its derivatives in cancer therapy. We select representative drug delivery systems involving LMWH derivatives and discuss the construction principles and therapeutic effects associated with their use. We also analyze progress made in the development of antitumor combination therapies, in which LMWH has shown synergistic or combined effects with other treatment strategies.
低分子量肝素 (LMWH) 因其广泛的生理功能而引起了人们对肿瘤治疗的越来越多的关注。在过去的十年中，各种 LMWH 衍生物增加了可用的抗肿瘤策略的多样性，不仅作为抗肿瘤剂，而且作为药物传递平台。在这篇综述中，我们介绍了 LMWH 结构修饰的基本策略，以减轻其抗肿瘤活性，同时降低其出血和免疫反应的风险，并强调了 LMWH 及其衍生物在癌症治疗中的当前应用。我们选择了涉及 LMWH 衍生物的代表性药物传递系统，并讨论了与它们的使用相关的构建原则和治疗效果。我们还分析了抗肿瘤联合治疗的发展进展，其中 LMWH 与其他治疗策略表现出协同或联合作用。
