Department of Urology, Lukas Hospital, Preussen Strasse 84, Neuss, Germany.
Anticancer Drugs. 2011 Jan;22(1):9-17. doi: 10.1097/CAD.0b013e3283404db0.
The novel third-generation bifluorinated semisynthetic vinca alkaloid, vinflunine, is a microtubule inhibitor that shows superior antitumor activity and a favorable safety profile compared with other vinca alkaloids. The main antineoplastic effects of vinflunine arise from its interaction with tubulin, the major component of microtubules in mitotic spindles. Vinflunine is known to have low affinity for tubulin, high intracellular accumulation, and important effects on microtubule dynamics. It has been shown to have activity against transitional cell carcinoma of the urothelial tract. Vinflunine was investigated in a randomized phase III clinical trial comparing vinflunine and best supportive care versus best supportive care alone in patients with advanced transitional cell carcinoma of the urothelial tract, who were progressive after first-line platinum-containing therapy. At an acceptable safety profile without cumulative toxicity, second-line treatment with vinflunine has shown a survival advantage and has therefore been approved in 2009 for this indication. This review gives a brief outline on vinflunine as a second-line treatment for platin-resistant advanced urothelial carcinoma; it describes pharmacology, efficacy studies, tolerance, and side effects and briefly discusses future clinical perspectives.
新型第三代双氟半合成长春碱类药物长春氟宁是一种微管抑制剂,与其他长春碱类药物相比,具有更好的抗肿瘤活性和良好的安全性。长春氟宁的主要抗肿瘤作用源于其与微管的主要成分——有丝分裂纺锤体中的微管蛋白的相互作用。长春氟宁与微管蛋白的亲和力低,细胞内蓄积率高,对微管动力学有重要影响。已证实其对尿路上皮移行细胞癌有活性。长春氟宁曾在一项随机 III 期临床试验中进行研究,该试验将长春氟宁联合最佳支持治疗与单纯最佳支持治疗进行比较,用于一线含铂化疗后进展的晚期尿路上皮移行细胞癌患者。二线治疗采用长春氟宁,在可接受的安全性且无累积毒性的情况下,显示出生存优势,因此在 2009 年批准用于该适应证。本文简要概述了长春氟宁作为铂类耐药性晚期尿路上皮癌的二线治疗药物,介绍了其药理学、疗效研究、耐受性和副作用,并简要讨论了未来的临床前景。