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卡博替尼作为晚期肾细胞癌的一线治疗:其应用概述

Cabozantinib as first-line treatment in advanced renal cell carcinoma: a profile of its use.

作者信息

Lyseng-Williamson Katherine A

机构信息

Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754 New Zealand.

出版信息

Drugs Ther Perspect. 2018;34(10):457-465. doi: 10.1007/s40267-018-0547-6. Epub 2018 Aug 7.

Abstract

Oral cabozantinib tablets (Cabometyx) are an important option for the treatment of advanced renal cell carcinoma (RCC). Cabozantinib is an anti-angiogenic agent and potently inhibits multiple tyrosine kinases, including those implicated in the development of RCC. The previously approved indication of cabozantinib tablets (i.e. treatment of advanced RCC following prior VEGF-targeted therapy) has been extended to include the first-line treatment of advanced RCC in treatment-naïve adults with intermediate or poor risk (EU) and all patients with advanced RCC (USA). These label extensions are based on the results of a randomized, open-label phase 2 trial, in which adults with metastatic RCC of poor or intermediate risk received targeted first-line treatment with cabozantinib or standard-of-care sunitinib. Relative to sunitinib, cabozantinib significantly prolonged median progression-free survival (primary endpoint; investigator and independent assessments), and increased the objective response rate (investigator assessment). The tolerability profile of cabozantinib is comparable to those of other tyrosine kinase inhibitors, with adverse events being manageable with medical intervention, dosage reductions, treatment interruption and/or permanent discontinuation.

摘要

口服卡博替尼片(Cabometyx)是治疗晚期肾细胞癌(RCC)的重要选择。卡博替尼是一种抗血管生成药物,能有效抑制多种酪氨酸激酶,包括那些与RCC发生发展相关的激酶。卡博替尼片先前已获批的适应症(即先前接受VEGF靶向治疗后的晚期RCC治疗)已扩展至包括一线治疗初治的中度或低度风险成年晚期RCC患者(欧盟)以及所有晚期RCC患者(美国)。这些标签扩展基于一项随机、开放标签的2期试验结果,在该试验中,中度或低度风险的转移性RCC成年患者接受了卡博替尼或标准治疗药物舒尼替尼的一线靶向治疗。相对于舒尼替尼,卡博替尼显著延长了中位无进展生存期(主要终点;研究者和独立评估),并提高了客观缓解率(研究者评估)。卡博替尼的耐受性与其他酪氨酸激酶抑制剂相当,不良事件可通过医学干预、剂量减少、治疗中断和/或永久停药来控制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ccec/6323107/a6ad4581b107/40267_2018_547_Fig1_HTML.jpg

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