[靶向酪氨酸激酶的抗肿瘤药物]

[Antineoplastic agents targeting tyrosine kinases].

作者信息

Guren Tormod K, Christoffersen Thoralf, Thoresen G Hege, Wisløff Finn, Dajani Olav, Tveit Kjell M

机构信息

Farmakologisk institutt, Rikshospitalet, Universitetet i Oslo, Postboks 1057 Blindern, 0316 Oslo.

出版信息

Tidsskr Nor Laegeforen. 2005 Nov 17;125(22):3115-9.

PMID:16299568

Abstract

BACKGROUND

Drugs that target tyrosine kinases belong to a new class of antineoplastic therapeutics, directed at cellular signalling mechanisms. Notes on the use of these agents and some of the clinical data are discussed in this review.

METHODS

The article is based on a review of recent literature and the authors' personal experience.

RESULTS AND INTERPRETATION

Receptor tyrosine kinases and intracellular tyrosine kinases regulate cellular events that may be involved in tumour development, such as proliferation, survival, and angiogenesis. Some of these agents are established in clinical practice, in particular the small-molecular tyrosine kinase inhibitor imatinib in the treatment of chronic myeloid leukaemia and gastrointestinal stromal tumours and the antibody trastuzumab in the treatment of breast cancer. Inhibitors of epidermal growth factor receptor (EGFR) and other tyrosine kinases are either established in clinical practice or under clinical investigation.

摘要

背景

靶向酪氨酸激酶的药物属于一类新型抗肿瘤治疗药物，作用于细胞信号传导机制。本文综述了这些药物的使用注意事项及部分临床数据。

方法

本文基于近期文献综述及作者个人经验撰写。

结果与解读

受体酪氨酸激酶和细胞内酪氨酸激酶调节细胞活动，这些活动可能参与肿瘤发展，如增殖、存活和血管生成。其中一些药物已在临床实践中得到应用，特别是小分子酪氨酸激酶抑制剂伊马替尼用于治疗慢性髓性白血病和胃肠道间质瘤，以及抗体曲妥珠单抗用于治疗乳腺癌。表皮生长因子受体（EGFR）和其他酪氨酸激酶抑制剂已在临床实践中应用或正在进行临床研究。