Ceulemans F, Humblet Y, Bosly A, Symann M, Trouet A
Cancer Chemother Pharmacol. 1986;18(1):44-6. doi: 10.1007/BF00253062.
Vinblastine tryptophan ester (VTrpE) is a new vinca alkaloid derivative that achieves antitumor activity in a large variety of animal models. In this phase I study the drug was given as an i.v. injection over 5 min, once a week or once every 2 weeks. Twenty patients with advanced cancer were entered in this trial. The doses ranged from 2.5 mg/m2 to 35 mg/m2. Myelosuppression is the dose-limiting toxicity, with the risk of leukopenia being more serious than that of thrombocytopenia, but the myelosuppression is always reversible. Neurotoxicity, well documented when other vinca alkaloid derivatives are used, is insignificant. Two cases of disease stabilization have been observed in patients with non-small cell lung cancer. For VTrpE, a dose schedule of 30 mg/m2 per week may be recommended for phase II studies in non-small cell lung cancer.
长春碱色氨酸酯（VTrpE）是一种新型长春花生物碱衍生物，在多种动物模型中均具有抗肿瘤活性。在这项I期研究中，该药物通过静脉注射给药，持续5分钟，每周一次或每两周一次。20例晚期癌症患者参与了该试验。剂量范围为2.5mg/m²至35mg/m²。骨髓抑制是剂量限制性毒性，白细胞减少的风险比血小板减少更严重，但骨髓抑制总是可逆的。使用其他长春花生物碱衍生物时记录充分的神经毒性并不明显。在非小细胞肺癌患者中观察到2例病情稳定。对于VTrpE，在非小细胞肺癌的II期研究中，可能推荐每周30mg/m²的给药方案。
