Department of Physiology and Pharmacology, Sackler School of Medicine, Room 607, Tel Aviv University, Tel Aviv 69978, Israel.
Adv Drug Deliv Rev. 2009 Nov 12;61(13):1159-76. doi: 10.1016/j.addr.2009.06.005. Epub 2009 Aug 20.
Angiogenesis, the formation of new blood vessels from pre-existing vasculature, is one of the central key steps in tumor progression and metastasis. Consequently, it became an important target in cancer therapy, making novel angiogenesis inhibitors a new modality of anticancer agents. Although relative to conventional chemotherapy, anti-angiogenic agents display a safer toxicity profile, the vast majority of these agents are low-molecular-weight compounds exhibiting poor pharmacokinetic profile with short half-life in the bloodstream and high overall clearance rate. The "Polymer Therapeutics" field has significantly improved the therapeutic potential of low-molecular-weight drugs and proteins for cancer treatment. Drugs can be conjugated to polymeric carriers that can be either directly conjugated to targeting proteins or peptides or derivatized with adapters conjugated to a targeting moiety. This approach holds a significant promise for the development of new targeted anti-angiogenic therapies as well as for the optimization of existing anti-angiogenic drugs or polypeptides. Here we overview the innovative approach of targeting tumor angiogenesis using polymer therapeutics.
血管生成，即从预先存在的脉管系统中形成新的血管，是肿瘤进展和转移的核心关键步骤之一。因此，它成为癌症治疗的一个重要靶点，使新型血管生成抑制剂成为一种新的抗癌药物模式。尽管与传统化疗相比，抗血管生成剂显示出更安全的毒性特征，但这些药物绝大多数是低分子量化合物，在血液中的半衰期短，整体清除率高，药代动力学特征不佳。“聚合物治疗学”领域极大地提高了低分子量药物和蛋白质治疗癌症的治疗潜力。药物可以与聚合物载体连接，聚合物载体可以直接与靶向蛋白或肽连接，也可以通过与靶向部分连接的接头衍生化。这种方法为开发新的靶向抗血管生成疗法以及优化现有的抗血管生成药物或多肽提供了巨大的潜力。在这里，我们概述了使用聚合物治疗学靶向肿瘤血管生成的创新方法。
