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长春氟宁:一种新型微管抑制剂。

Vinflunine: a new microtubule inhibitor agent.

作者信息

Bennouna Jaafar, Delord Jean-Pierre, Campone Mario, Nguyen Laurent

机构信息

Centre René Gauducheau, Saint-Herblain, France.

出版信息

Clin Cancer Res. 2008 Mar 15;14(6):1625-32. doi: 10.1158/1078-0432.CCR-07-2219.

Abstract

Vinflunine (Javlor) is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine is obtained by semisynthesis using superacidic chemistry to selectively introduce two fluorine atoms at the 20' position of the catharanthine moiety. This compound has been selected for clinical development on the basis of encouraging preclinical activity that warrants study in patients with a wide spectrum of solid tumors. Clinically significant activity has been seen in phase II studies, mainly in the treatment of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast. Vinflunine is currently in phase III trial assessment in patients with (second line) transitional cell carcinoma of the urothelium and first-line advanced breast cancer. The efficacy of vinflunine in patients with advanced non-small cell lung cancer previously treated with a platinum-containing regimen was confirmed by a large phase III trial.

摘要

长春氟宁(Javlor)是首个属于长春花生物碱家族的氟化微管抑制剂。长春氟宁通过半合成获得,利用超强酸化学方法在长春碱部分的20'位选择性引入两个氟原子。基于令人鼓舞的临床前活性,该化合物被选用于临床开发,这种活性保证了对广泛实体瘤患者进行研究的必要性。在II期研究中已观察到具有临床意义的活性,主要用于治疗尿路上皮移行细胞癌、非小细胞肺癌和乳腺癌。长春氟宁目前正处于III期试验评估阶段,用于治疗(二线)尿路上皮移行细胞癌和一线晚期乳腺癌患者。一项大型III期试验证实了长春氟宁对先前接受含铂方案治疗的晚期非小细胞肺癌患者的疗效。

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