Lobert Sharon, Puozzo Christian
University of Mississippi Medical Center, Jackson, MS, USA.
Semin Oncol. 2008 Jun;35(3 Suppl 3):S28-33. doi: 10.1053/j.seminoncol.2008.01.007.
The novel microtubule inhibitor, vinflunine, has a unique mechanism of action that differs from other members of the vinca alkaloid class in terms of tubulin-binding affinity, microtubule dynamics, spiral formation, and intracellular accumulation. Vinflunine has shown significant activity in vivo, which involves its antimitotic, antiangiogenic, and antivascular properties. The promising preclinical activity of vinflunine has warranted further investigation in the clinical setting. This review explores the distinct interaction of vinflunine with its intracellular targets to gain insight into its mechanism of action and safety profile. The pharmacokinetic properties and metabolism of vinflunine in animals and in human subjects are also discussed, together with an analysis of potential drug-drug interactions and the influence of age, liver dysfunction, or renal dysfunction on the overall activity of vinflunine.
新型微管抑制剂长春氟宁具有独特的作用机制，在微管蛋白结合亲和力、微管动力学、螺旋形成和细胞内蓄积方面与长春花生物碱类的其他成员不同。长春氟宁在体内已显示出显著活性，涉及其抗有丝分裂、抗血管生成和抗血管特性。长春氟宁有前景的临床前活性值得在临床环境中进一步研究。本综述探讨长春氟宁与其细胞内靶点的独特相互作用，以深入了解其作用机制和安全性概况。还讨论了长春氟宁在动物和人类受试者中的药代动力学特性及代谢，同时分析了潜在的药物相互作用以及年龄、肝功能障碍或肾功能障碍对长春氟宁整体活性的影响。
