Cabozantinib: Mechanism of action, efficacy and indications
Cabozantinib: Mechanism of action, efficacy and indications
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DOI：
10.1016/j.bulcan.2017.03.013
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发表时间：
2017-05-01
影响因子：
1.2
通讯作者：
Le Moulec, Sylvestre
中科院分区：
文献类型：
--
作者：
Cochin, Valerie;Gross-Goupil, Marine;Le Moulec, Sylvestre
Cabozantinib是一种口服多酪氨酸激酶受体抑制剂（ITK）：VEGFR 2，c-MET和RET。VEGFR和c-MET的抑制通过c-MET轴降低VEGFR抑制剂的耐药性。卡博替尼改善进行性转移性甲状腺髓样癌（MTC）的无进展生存期（PFS）：在所有患者亚组中，安慰剂组为4个月，卡博替尼组为11.2个月（P < 0.001），包括具有或不具有先前ITK和RET突变状态的那些患者亚组。与依维莫司相比，卡博替尼增加了先前VEGFR ITK治疗后进展的晚期肾细胞癌患者的总生存期（OS）：卡博替尼组为21.4个月，依维莫司组为16.5个月（P < 0.0003）。卡博替尼获得AMM用于治疗进行性转移性MTC和晚期肾细胞癌。卡博替尼是治疗MTC的一种新选择，包括治疗试验（在该适应症中不支付）和晚期肾细胞癌（住院分娩）。其耐受性与抗血管生成疗法相似，证明了对继发性效应的最佳管理是合理的。
Cabozantinib is an oral multiple tyrosine kinase receptor inhibitor (ITK): VEGFR2, c-MET and RET. Inhibition of VEGFR and c-MET decrease resistance of VEGFR inhibitor via c-MET axis. Cabozantinib improve progression-free survival (PFS) in progressive metastatic medullary thyroid cancer (MTC): 4 months in the placebo group and 11.2 months in the cabozantinib group (P < 0.001) in all patient subgroups including those with or without prior ITK and RET mutation status. Cabozantinib increased overall survival (OS) compared with everolimus in patients with advanced renal cell carcinoma who progressed after previous VEGFR ITK treatment: 21.4 months in cabozantinib group and 16.5 months in everolimus group (P < 0.0003). Cabozantinib obtained the AMM for the treatment of progressive metastatic MTC and advanced renal cell carcinoma. Cabozantinib is a new option in the treatment of MTC by inclusion in therapeutic trials (no payment in this indication) and advanced renal cell carcinoma (hospital delivery). Its tolerance is similar to anti-angiogenic therapies and justifies an optimal management of the secondary effect.