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。
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 Ⅱ and 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.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2008年第12期1541-1544,共4页
Chinese Pharmacological Bulletin