Ito Yoshinori, Tokudome Nahomi, Sugihara Tsutomu, Takahashi Shunji, Hatake Kiyohiko
Department of Medical Oncology, Cancer Institute Hospital, Japanese Foundation for Cancer Research, Japan.
Breast Cancer. 2007;14(2):156-62. doi: 10.2325/jbcs.971.
ErbB/HER receptor or its signal transduction pathway is an attractive therapeutic target for breast cancer. Lapatinib, an orally administered dual inhibitor of ErbB1 (EGFR) and ErbB2 (HER2) receptor tyrosine kinases has shown promising results for metastatic breast cancer (MBC). Lapatinib exhibited activity against trastuzumab-refractory MBC and showed an acceptable adverse event profile such as transient mild rash, diarrhea and nausea. The addition of lapatinib to capecitabine resulted in significantly prolonged time to progression. Large randomized trials using lapatinib following chemotherapy and surgery are ongoing for early stage HER2-overexpressing breast cancer. Various combinations with agents such as paclitaxel, aromatase inhibitors, or other molecular targeted agents are currently being investigated in clinical trials. If these approaches overcome the limitations of trastuzumab, lapatinib will become an effective treatment option for breast cancer in the near future.
ErbB/HER受体或其信号转导通路是乳腺癌一个颇具吸引力的治疗靶点。拉帕替尼是一种口服的ErbB1（表皮生长因子受体，EGFR）和ErbB2（人表皮生长因子受体2，HER2）受体酪氨酸激酶双重抑制剂，已在转移性乳腺癌（MBC）的治疗中显示出良好效果。拉帕替尼对曲妥珠单抗难治性MBC具有活性，且显示出可接受的不良事件谱，如短暂的轻度皮疹、腹泻和恶心。拉帕替尼联合卡培他滨可显著延长疾病进展时间。针对早期HER2过表达乳腺癌，在化疗和手术后使用拉帕替尼的大型随机试验正在进行。目前，在临床试验中正在研究拉帕替尼与紫杉醇、芳香化酶抑制剂或其他分子靶向药物等药物的各种联合应用。如果这些方法克服了曲妥珠单抗的局限性，拉帕替尼在不久的将来将成为乳腺癌的一种有效治疗选择。
