Axitinib: a review of its safety and efficacy in the treatment of adults with advanced renal cell carcinoma.
Axitinib: a review of its safety and efficacy in the treatment of adults with advanced renal cell carcinoma.
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DOI：
10.4137/cmo.s10594
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发表时间：
2013-10-29
期刊：
影响因子：
--
通讯作者：
Ravaud A
中科院分区：
文献类型：
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作者：
Gross-Goupil M;François L;Quivy A;Ravaud A
在过去的七年中，七种靶向药物已被批准用于治疗晚期或转移性肾细胞癌，极大地改变了该疾病的治疗方法和预后。已证实有效的最新药物是阿西替尼（Inlyta®）。这种新一代酪氨酸激酶药物与先前存在的药物的不同之处在于其抑制血管内皮生长因子受体（VEGFR1 - 3）的活性更强。这种功效已在II期和III期临床试验中得到测试。阿昔替尼是唯一受益于推荐滴定的靶向药物，患者内剂量递增。该药物的毒性特征是可耐受的。本文综述了阿西替尼的作用机制、代谢和药代动力学特征。还详细介绍了疗效和安全性的临床数据。该药物已被纳入国际治疗指南，作为治疗肾细胞癌患者的标准，以前通过抗血管生成治疗。
Over the last seven years, seven targeted agents have been approved in the treatment of advanced or metastatic renal cell cancer, changing the therapeutic approach and prognosis of the disease dramatically. The latest agent with demonstrated efficacy is axitinib (Inlyta®). This new generation of tyrosine kinase agent differs from previously existing agents by its greater activity potency of inhibition of vascular endothelial growth factor-receptor (VEGFR1-3). This efficacy has been tested in phase II and III clinical trials. Axitinib is the only targeted agent that benefits from recommended titration, with intra-patient dose escalation. The toxicity profile of the drug is tolerable. This paper reviews the mechanism of action of axitinib, its metabolism, and its pharmacokinetic profile. Clinical data of efficacy and safety is also detailed. The agent has been integrated in the international therapeutic guidelines, as a standard in treatment of renal cell cancer patients, previously treated through antiangiogenic therapy.