Kessler E R, Bowles D W, Flaig T W, Lam E T, Jimeno A
University of Colorado School of Medicine, Division of Medical Oncology, Denver, Colorado 80045, USA.
Drugs Today (Barc). 2012 Oct;48(10):633-44. doi: 10.1358/dot.2012.48.10.1860768.
Axitinib is a small-molecule protein-tyrosine kinase receptor inhibitor specifically targeting this family of receptors, in addition to platelet-derived growth factor receptor and proto-oncogene c-Kit. Improved knowledge of kidney cancer development, and specifically mutations in the VHL gene, has supported the targeting of angiogenesis pathways. Axitinib is the most recently approved agent for use in metastatic renal cell carcinoma. This review will focus on the preclinical pharmacology, pharmacokinetics and clinical activity of this agent, and describe its place in the current treatment of renal cell carcinoma.
阿昔替尼是一种小分子蛋白酪氨酸激酶受体抑制剂，除了靶向血小板衍生生长因子受体和原癌基因c-Kit外，还特异性靶向该受体家族。对肾癌发展，特别是VHL基因突变的深入了解，支持了对血管生成途径的靶向治疗。阿昔替尼是最近被批准用于转移性肾细胞癌的药物。本综述将聚焦于该药物的临床前药理学、药代动力学和临床活性，并描述其在当前肾细胞癌治疗中的地位。
