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凡德他尼是一种抑制血管内皮生长因子受体-2(VEGFR-2)、表皮生长因子受体(EGFR)和转染重排(RET)酪氨酸激酶活性的新型口服活性拮抗剂,于2011年4月6日获得美国食品与药品管理局(FDA)批准用于治疗甲状腺髓样癌(MTC)。文中综述了凡德他尼的药代动力学和药效学,重点介绍了其对MTC进行的II～III期临床试验的疗效和单用或与化疗药物联用对非小细胞肺癌(NSCLC)患者进行4项III期临床试验和部分其他II期临床试验的结果。同时,对其在MTC和NSCLC的III期临床试验中的效果和不良反应进行了评价和讨论。此外,凡德他尼单用或与其他药合用对前列腺癌患者、晚期乳腺癌患者和恶性胶质瘤患者进行的II期试验已完成;而对胆管癌、尿道肿瘤和肾癌的II期临床试验正在征集受试者。这些试验的结果将能更好地确定凡德他尼的适当治疗方案、评价的最佳人群和长期使用凡德他尼的安全性等。
Vandetanib is a novel, orally active antagonist that inhibits the activity of vascular endothelial growth factor receptor-2 (VEGFR-2), epidermal growth factor receptor (EGFR) and transfection rearrangement (RET) tyrosine kinases, On April 6, 2011, the United States Food and Drug Administration (FDA) approved for the treatment of medullary thyroid carcinoma (MTC). In this review, the pharmacokinetics and pharmacodynamics of vandetanib are reviewed. The efficacy of vandetanib in phase II-III clinical trials and the combination with chemotherapeutics on non-small cell lung cancer (NSCLC) Patients performed the results of 4 phase III clinical trials and some of the other phase II clinical trials. At the same time, its efficacy and adverse reactions in MTC and NSCLC phase III clinical trials were evaluated and discussed. In addition, Phase II trials of vandetanib alone or in combination with other medications for patients with prostate cancer, advanced breast cancer and glioblastoma have been completed; whereas Phase II trials of cholangiocarcinoma, urethral neoplasms and renal cancer The trial is collecting the subjects. The results of these trials will allow for a better determination of the appropriate treatment of vandetanib, the evaluation of the optimal population and the safety of long-term use of vandetanib.