Endocrinology Unit, Department of Clinical & Experimental Medicine, WHO Collaborating Center for the Study & Treatment of Thyroid Diseases & other Endocrine & Metabolic Disorders, University of Pisa, Via Paradisa 2, Pisa 56124, Italy.
Future Oncol. 2013 Aug;9(8):1083-92. doi: 10.2217/fon.13.128.
Cabozantinib (XL184) is an oral multiple receptor tyrosine kinase inhibitor manufactured by Exelixis Inc., CA, USA. It mainly inhibits three tyrosine kinase receptors: MET, VEGFR2 and RET. In both preclinical and clinical studies it has been shown to inhibit tumor angiogenesis, invasiveness and metastases. The most frequent side effects are fatigue, diarrhea, decreased appetite, nausea, weight loss and palmar-plantar erythrodysesthesia. A Phase III clinical trial (EXAM study) of XL184 versus placebo in advanced and progressive medullary thyroid cancer showed a 28 versus 0% overall response rate and a progression-free survival of 11.2 versus 4.0 months (hazard ratio: 0.28; 95% CI: 0.19-0.40; p < 0.0001) in patients treated with cabozantinib and placebo, respectively. The drug has been approved by the US FDA for the treatment of advanced/progressive metastatic medullary thyroid cancer in the USA. The EMA is now evaluating its approval in Europe.
卡博替尼（XL184）是一种由美国加利福尼亚州 Exelixis 公司生产的口服多受体酪氨酸激酶抑制剂。它主要抑制三种酪氨酸激酶受体：MET、VEGFR2 和 RET。在临床前和临床研究中，它已被证明能抑制肿瘤血管生成、侵袭和转移。最常见的副作用是疲劳、腹泻、食欲下降、恶心、体重减轻和掌跖红细胞感觉异常。一项比较 XL184 与安慰剂治疗晚期和进展性甲状腺髓样癌的 III 期临床试验（EXAM 研究）显示，卡博替尼组的总缓解率为 28%，而安慰剂组为 0%；无进展生存期分别为 11.2 个月和 4.0 个月（风险比：0.28；95%CI：0.19-0.40；p<0.0001）。该药物已获得美国 FDA 批准用于治疗美国晚期/进展性转移性甲状腺髓样癌。EMA 目前正在评估其在欧洲的批准情况。
