Dipartimento di Medicina Interna e Specialità Mediche, Sapienza Università di Roma, V.le del Policlinico, 155, 00161, Rome, Italy.
Endocrine. 2013 Oct;44(2):334-42. doi: 10.1007/s12020-013-9943-9. Epub 2013 Apr 14.
Medullary thyroid cancer (MTC) is frequently diagnosed in a locally advanced or metastatic stage, and 10-year survival rates in these cases are below 20 %. Cytotoxic chemotherapy has no significant impact on overall or progression-free survival. Vandetanib (Caprelsa(®), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60 % of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors. It is the first systemic drug with demonstrated anti-tumor benefits in advanced MTC, and it has recently been approved for locally advanced or metastatic MTC by the United States Food and Drug Administration (April 2011) and the European Medicines Agency (February 2012). This review, starting from the phases II and III efficacy and safety data that led to these approvals, explores important issues related to dosing, patient selection, and strategies for managing the substantial risk of toxicity associated with the drug (including life-threatening cardiac events that are the subject of a black-box warning in the United States). All these issues still remain to be defined. Vandetanib is becoming a standard of care for symptomatic, progressive, metastatic MTCs, to be used selectively in those patients who are likely to benefit from it.
甲状腺髓样癌(MTC)常发生于局部晚期或转移阶段,这些情况下的 10 年生存率低于 20%。细胞毒性化疗对总生存期或无进展生存期无显著影响。凡德他尼(Caprelsa®,阿斯利康)是一种每日一次的口服酪氨酸激酶抑制剂,选择性抑制生长因子受体酪氨酸激酶 RET(在大约 60%的所有 MTC 中均为持续激活)、血管内皮生长因子受体 2 和 3 以及表皮生长因子受体的信号转导。它是第一种在晚期 MTC 中具有明确抗肿瘤益处的全身药物,最近已被美国食品和药物管理局(2011 年 4 月)和欧洲药品管理局(2012 年 2 月)批准用于局部晚期或转移性 MTC。本文从导致这些批准的 II 期和 III 期疗效和安全性数据出发,探讨了与剂量、患者选择和管理与药物相关的毒性的大量风险(包括危及生命的心脏事件,在美国被列为黑框警告)相关的重要问题。所有这些问题仍有待确定。凡德他尼正在成为有症状、进展性、转移性 MTC 的治疗标准,将选择性地用于那些可能从中受益的患者。