| EGFR/HER-2双受体酪氨酸激酶抑制剂拉帕替尼的研究进展 |
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| 引用本文： | 陶黎阳,符立梧. EGFR/HER-2双受体酪氨酸激酶抑制剂拉帕替尼的研究进展[J]. 中国药理学通报, 2008, 24(12) |
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| 作者姓名： | 陶黎阳 符立梧 |
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| 作者单位： | 华南肿瘤学国家重点实验室,中山大学肿瘤防治中心,广东,广州,510060 |
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| 摘 要： | EGFR/HER-2是理想的抗肿瘤分子靶点。拉帕替尼(lapatinib)是口服的小分子EGFR/HER-2双受体酪氨酸激酶抑制剂,体内外的临床前试验证实了lapatinib的抗肿瘤活性,Ⅰ期临床研究显示了它的安全性,治疗侵袭、复发、炎性、脑转移乳癌的Ⅱ、Ⅲ期临床研究取得了可喜的成绩。随着对乳癌生物特性的理解,选择特异的肿瘤亚型(HER-2过表达),进行分子靶向治疗(例如lapatinib)正成为一种新的辅助治疗方案。
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| 关 键 词： | lapatinib 上皮生长因子受体家族 乳腺癌 |
Progress of study on lapatinib |
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| TAO Li-yang,FU Li-wu. Progress of study on lapatinib[J]. Chinese Pharmacological Bulletin, 2008, 24(12) |
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| Authors: | TAO Li-yang FU Li-wu |
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| Affiliation: | TAO Li-yang,FU Li-wu(State Key Laboratory of Oncology in South China,Cancer Center,Sun Yat-sen University,Guangzhou 510060,China) |
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| Abstract: | EGFR/HER-2 is an attractive therapeutic target for solid tumors.Lapatinib is an orally administered dual inhibitor of EGFR/HER-2 tyosine kinases.Preclinical experiments in vitro and in vivo models indicate that lapatinib is active against various solid tumors.Phase Ⅰ trials have shown an acceptable adverse event.Phase Ⅱand Ⅲ trials demonstrate the promising results for the treatment of metastatic,refractory,inflammatory,or brain metastatic breast cancer.With the further developments of biology,the molecular targeted chemotherapy becomes a novel adjuvant therapy for advanced breast cancer patients. |
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| Keywords: | lapatinib |
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