Moy Beverly, Goss Paul E
Massachusetts General Hospital Cancer Center, Boston, Massachusetts 02114, USA.
Oncologist. 2006 Nov-Dec;11(10):1047-57. doi: 10.1634/theoncologist.11-10-1047.
Lapatinib is an oral receptor tyrosine kinase inhibitor, targeting both the ErbB-1 and ErbB-2 receptors. Pre-clinical in vitro and in vivo models indicate that lapatinib is active as monotherapy, synergistically in combination with trastuzumab, and in trastuzumab-resistant cell lines. Early clinical trials also provide evidence in patients that lapatinib is active against breast cancer. This paper reviews results of phase II and III clinical trials of lapatinib in metastatic breast cancer, evidence for its potential in patients with brain metastases, and current clinical trials as adjuvant treatment in early-stage disease. Our improved understanding of the biology of breast cancer and the use of biomarkers for identification of specific subtypes is allowing us to bring patient-specific novel therapies such as lapatinib to the clinic.
拉帕替尼是一种口服受体酪氨酸激酶抑制剂，可同时靶向表皮生长因子受体-1（ErbB-1）和表皮生长因子受体-2（ErbB-2）。临床前的体外和体内模型表明，拉帕替尼作为单一疗法具有活性，与曲妥珠单抗联合使用具有协同作用，并且在曲妥珠单抗耐药的细胞系中也有活性。早期临床试验也为患者提供了证据，证明拉帕替尼对乳腺癌有效。本文综述了拉帕替尼治疗转移性乳腺癌的II期和III期临床试验结果、其在脑转移患者中的潜在证据以及目前作为早期疾病辅助治疗的临床试验。我们对乳腺癌生物学的深入理解以及使用生物标志物来识别特定亚型，使我们能够将拉帕替尼等针对患者的新型疗法引入临床。
