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酪氨酸激酶抑制剂:选择性、敏感性和临床性能的观点。

Tyrosine kinase inhibitors: views of selectivity, sensitivity, and clinical performance.

机构信息

Unit of Cellular Signaling, Department of Biological Chemistry, Alexander Siberman Institute of Life Sciences, Hebrew University of Jerusalem, Jerusalem 91904 Israel.

出版信息

Annu Rev Pharmacol Toxicol. 2013;53:161-85. doi: 10.1146/annurev-pharmtox-011112-140341. Epub 2012 Oct 8.

Abstract

With the manufacture of imatinib, researchers introduced tyrosine kinase inhibitors (TKIs) into the clinical setting in 2000 to treat cancers; approximately fifteen other TKIs soon followed. Imatinib remains the most successful agent, whereas all the others have had modest effects on the cancers that they target. The current challenge is to identify the agents that need to be combined with TKIs to maximize their efficacy. One of the most promising approaches is to combine immune therapy with TKI treatment. In this review, the therapeutic potential of TKIs for treatment is discussed.

摘要

随着伊马替尼的制造,研究人员于 2000 年将酪氨酸激酶抑制剂(TKI)引入临床应用,以治疗癌症;此后不久,又出现了大约十五种其他 TKI。伊马替尼仍然是最成功的药物,而其他所有药物对其靶向的癌症只有适度的疗效。目前的挑战是确定需要与 TKI 联合使用以最大程度提高其疗效的药物。最有前途的方法之一是将免疫疗法与 TKI 治疗相结合。在这篇综述中,讨论了 TKI 治疗的治疗潜力。

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