来那替尼单药或联合治疗 HER2 阳性乳腺癌的作用。
Role of lapatinib alone or in combination in the treatment of HER2-positive breast cancer.
机构信息
Department of Medicine, University of California, Los Angeles, CA, USA.
出版信息
Breast Cancer (Dove Med Press). 2012 Apr 3;4:35-51. doi: 10.2147/BCTT.S29996.
PURPOSE
This review aims to present the preclinical and clinical data regarding efficacy and safety of lapatinib alone and in combination with other agents in the treatment of human epidermal growth factor receptor-2 (HER2)-overexpressing breast cancer.
BACKGROUND
HER2-positive (HER2+) breast cancer remains a treatment challenge. It is more aggressive than other breast cancers and it is associated with a poor outcome. Targeted therapy for HER2+ breast cancer has significantly changed the clinical course of the disease. Despite advances in therapy, there remains an unmet need in the treatment of HER2+ breast cancer. Lapatinib is a novel, orally bioavailable epidermal growth factor receptor/HER2+ targeted agent. Many trials have investigated the efficacy and safety of lapatinib alone and in conjunction with other agents in the treatment of HER2+ breast cancer.
METHODS AND RESULTS
Preclinical and clinical trials of lapatinib have shown that it is effective in the treatment on HER2+ breast cancer. More important, studies show that it is effective in the setting of trastuzumab resistance and in the treatment of central nervous system metastases, both of which are current treatment challenges. Furthermore, lapatinib is effective in conjunction with trastuzumab in the treatment of early breast cancer. Data regarding the safety of lapatinib show that it is generally well tolerated; however, multiple studies have shown significant (grade 3 and 4) diarrhea and rash associated with lapatinib, thereby limiting its use. Carditoxicity has not been a significant adverse event associated with the use of lapatinib.
CONCLUSION
Lapatinib is effective alone and in conjunction with other agents in the treatment of HER2+ breast cancer. However, its use is limited by significant diarrhea and rash.
目的
本篇综述旨在介绍拉帕替尼单独或联合其他药物治疗人表皮生长因子受体 2（HER2）过表达乳腺癌的临床前和临床疗效及安全性数据。
背景
HER2 阳性（HER2+）乳腺癌仍然是一个治疗挑战。与其他乳腺癌相比，它具有侵袭性，预后较差。针对 HER2+乳腺癌的靶向治疗显著改变了疾病的临床病程。尽管治疗取得了进展，但 HER2+乳腺癌的治疗仍存在未满足的需求。拉帕替尼是一种新型、口服生物利用的表皮生长因子受体/HER2 靶向药物。许多试验已经研究了拉帕替尼单独和联合其他药物治疗 HER2+乳腺癌的疗效和安全性。
方法和结果
临床前和临床试验表明，拉帕替尼治疗 HER2+乳腺癌有效。更重要的是，研究表明，它在曲妥珠单抗耐药和治疗中枢神经系统转移方面有效，这两者都是目前的治疗挑战。此外，拉帕替尼与曲妥珠单抗联合治疗早期乳腺癌有效。关于拉帕替尼安全性的数据表明，它通常具有良好的耐受性；然而，多项研究表明，拉帕替尼与严重（3 级和 4 级）腹泻和皮疹相关，从而限制了其使用。心脏毒性不是使用拉帕替尼的一个显著不良事件。
结论
拉帕替尼单独或联合其他药物治疗 HER2+乳腺癌有效。然而，其严重腹泻和皮疹限制了其应用。
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