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喜树碱类

The camptothecins.

作者信息

Pizzolato Joseph F, Saltz Leonard B

机构信息

Memorial Sloan-Kettering Cancer Center, Gastrointestinal Oncology Service, 1275 York Avenue, New York, NY 10021, USA.

出版信息

Lancet. 2003 Jun 28;361(9376):2235-42. doi: 10.1016/S0140-6736(03)13780-4.

Abstract

Supported by detailed understanding of their mechanism of action, and facilitated by chemical manipulations that have amplified their solubility, the camptothecins have advanced to the forefront of several areas of therapeutic and developmental chemotherapy. Additive and synergistic laboratory interactions with other cytotoxic drugs have been exploited to allow development of camptothecin-based multidrug regimens, which are showing important activity in several malignancies. Topotecan and irinotecan are already in widespread use in clinical practice, and newer agents with promising preclinical activity are in various stages of clinical assessment. As knowledge of molecular and biochemical mechanisms of action and resistance continues to expand, newer and better camptothecin-based strategies for treatment of malignant disease are likely to evolve.

摘要

基于对其作用机制的详细了解,并借助提高其溶解度的化学操作,喜树碱类药物已在治疗性化疗和发育性化疗的多个领域中处于前沿地位。已利用其与其他细胞毒性药物在实验室中的相加和协同相互作用来开发基于喜树碱的多药方案,这些方案在多种恶性肿瘤中显示出重要活性。拓扑替康和伊立替康已在临床实践中广泛使用,具有有前景的临床前活性的新型药物正处于不同阶段的临床评估中。随着对分子和生化作用机制及耐药性的认识不断扩展,可能会演变出更新、更好的基于喜树碱的恶性疾病治疗策略。

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