Department of Oncology Hematology and Respiratory Diseases, University of Modena and Reggio Emilia University Hospital, Modena, Italy.
Expert Rev Anticancer Ther. 2009 Nov;9(11):1549-57. doi: 10.1586/era.09.124.
Lapatinib is an oral, small-molecule dual inhibitor of human EGF receptor 1 (EGFR/erbB1) and 2 (HER2/erbB2). Lapatinib has recently been approved, in combination with capecitabine, for the treatment of HER2-positive metastatic breast cancer patients failing trastuzumab therapy. Data from clinical trials are consistently showing the key role of this agent in the management of HER2-positive disease. Moreover, interesting data are suggesting a key role of lapatinib in enhancing endocrine responsiveness and/or restoring endocrine sensitivity in hormone receptor-positive disease. The present article will summarize the main data leading to the clinical development of the combination of lapatinib and the aromatase inhibitor letrozole.
拉帕替尼是一种口服的小分子双重抑制剂，可抑制人表皮生长因子受体 1（EGFR/erbB1）和 2（HER2/erbB2）。拉帕替尼最近已被批准与卡培他滨联合用于治疗曲妥珠单抗治疗失败的 HER2 阳性转移性乳腺癌患者。临床试验数据一直显示该药物在治疗 HER2 阳性疾病中的关键作用。此外，有趣的数据表明拉帕替尼在增强激素受体阳性疾病的内分泌反应性和/或恢复内分泌敏感性方面具有关键作用。本文将总结导致拉帕替尼与芳香酶抑制剂来曲唑联合应用的临床开发的主要数据。
