Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2010 Jul 9;70(10):1283-93. doi: 10.2165/11204970-000000000-00000.
Vinflunine is a novel bifluorinated vinca alkaloid that appears to differ from other class members in terms of its tubulin-binding properties and inhibitory effects on microtubule dynamics. Notably, it demonstrated superior in vivo antitumour activity to that of vinorelbine in a range of transplantable murine and human tumours. In a randomized, open-label, multicentre phase III trial in adult patients with advanced transitional cell carcinoma of the urothelium who experienced progression after first-line platinum-containing chemotherapy (n = 370), median overall survival (OS; primary endpoint) was 6.9 months for intravenous vinflunine plus best supportive care (BSC) recipients versus 4.6 months for BSC alone recipients in the intent to treat (ITT) population. The difference in OS between treatment groups was not significant in the ITT population; however, there was a significant improvement in OS for vinflunine plus BSC recipients in the ITT population after adjusting for prespecified prognostic factors, and in the analysis of the eligible population (ITT population excluding baseline protocol violations). In the latter, median OS was 6.9 months with vinflunine plus BSC versus 4.3 months with BSC alone after a median follow-up of approximately 1.8 years and again after a median follow-up of approximately 3.6 years. Progression-free survival, objective response rate and disease control rate were significantly improved with vinflunine plus BSC versus BSC alone. The most frequent treatment-related adverse events in vinflunine recipients included myelosuppression (e.g. neutropenia) and gastrointestinal symptoms (e.g. constipation). In general, adverse events with vinflunine were noncumulative and medically manageable.
长春氟宁是一种新型双氟取代长春碱类似物,在与微管结合特性和对微管动力学的抑制作用方面似乎与其他同类药物有所不同。值得注意的是,它在一系列可移植的鼠类和人类肿瘤中的体内抗肿瘤活性优于长春瑞滨。在一项针对接受过一线含铂化疗后进展的成人晚期尿路上皮移行细胞癌患者的随机、开放标签、多中心 III 期试验中(n = 370),静脉注射长春氟宁联合最佳支持治疗(BSC)组的中位总生存期(OS;主要终点)为 6.9 个月,而仅接受 BSC 组为 4.6 个月,在意向治疗(ITT)人群中。在 ITT 人群中,治疗组之间的 OS 差异无统计学意义;然而,在调整了预设预后因素后,在 ITT 人群中,长春氟宁联合 BSC 组的 OS 显著改善,在合格人群(排除基线方案违反的 ITT 人群)的分析中也是如此。在后一组中,中位 OS 为 6.9 个月,长春氟宁联合 BSC 组,而仅接受 BSC 组为 4.3 个月,中位随访时间约为 1.8 年,再次随访时间约为 3.6 年。长春氟宁联合 BSC 与 BSC 单药相比,无进展生存期、客观缓解率和疾病控制率均显著提高。长春氟宁组最常见的治疗相关不良事件包括骨髓抑制(如中性粒细胞减少症)和胃肠道症状(如便秘)。一般来说,长春氟宁的不良反应是非累积性的,且可通过医疗手段控制。