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甲状腺髓样癌(MTC)发生率占甲状腺癌的5%~8%,局部晚期或转移性MTC患者往往面临治疗手段选择有限和预后不良。酪氨酸激酶抑制剂(TKIs)为目前临床治疗MTC的新手段。Cabozantinib苹果酸盐是一种口服的多靶点的TKIs,临床前和临床的评价数据显示:它可以延长MTC患者的无进展生存期(PFS),且具有良好的耐受性。2012年11月Cabozantinib苹果酸盐被FDA批准用于进展性MTC的治疗。文章介绍了Cabozantinib的理化性质、作用机制、药动学参数、临床评价、药物相互作用和安全性等方面的内容。
Medullary thyroid carcinoma (MTC) incidence of thyroid cancer accounts for 5% to 8%, locally advanced or metastatic MTC patients often face limited choice of treatment and poor prognosis. Tyrosine kinase inhibitors (TKIs) for the clinical treatment of new means of MTC. Cabozantinib malate is an orally administered, multi-targeted TKIs. Preclinical and clinical evaluation data show that it prolongs the progression-free survival (PFS) of patients with MTC and is well tolerated. November 2012 Cabozantinib malate is FDA approved for the treatment of progressive MTC. This article describes the physical and chemical properties of Cabozantinib, mechanism of action, pharmacokinetic parameters, clinical evaluation, drug interactions and safety aspects.