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Lapatinib(拉帕替尼)是一种新型的口服双重酪氨酸激酶抑制剂(TKI),它能同时抑制表皮生长因子受体(EGFR)和表皮生长因子受体-2(HER-2)的酪氨酸激酶活性。Lapatinib的临床前期及临床研究结果表明:lapatinib在体外与活体试验中均显示有一定抗肿瘤活性。Lapatinib对乳腺癌患者,尤其对曲妥株单抗耐药的局部晚期和转移性乳腺癌患者显示了较好疗效。以lapatinib为代表的TKI有望为乳腺癌的治疗开辟一条崭新的途径。
Lapatinib is a novel oral dual tyrosine kinase inhibitor (TKI) that inhibits both epidermal growth factor receptor (EGFR) and epidermal growth factor receptor-2 (HER-2) Tyrosine kinase activity. Lapatinib preclinical and clinical studies have shown that: lapatinib in vitro and in vivo tests have shown some anti-tumor activity. Lapatinib shows good efficacy in patients with locally advanced and metastatic breast cancer who are resistant to breast cancer, especially to trastuzumab. The TKI, represented by lapatinib, is expected to open a new avenue for the treatment of breast cancer.