Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer?
Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer?
复制标题
DOI：
10.2325/jbcs.971
复制
发表时间：
2007-01-01
期刊：
影响因子：
--
通讯作者：
Hatake, Kiyohiko
中科院分区：
文献类型：
--
作者：
Ito, Yoshinori;Tokudome, Nahomi;Hatake, Kiyohiko
ErbB/HER受体或其信号转导途径是乳腺癌治疗的重要靶点。拉帕替尼是一种口服ErbB1 （EGFR）和ErbB2 （HER2）受体酪氨酸激酶的双重抑制剂，对转移性乳腺癌（MBC）显示出有希望的效果。拉帕替尼显示出抗曲妥珠单抗难治MBC的活性，并显示出可接受的不良事件，如短暂的轻度皮疹、腹泻和恶心。卡培他滨加用拉帕替尼可显著延长进展时间。在化疗和手术后使用拉帕替尼治疗早期her2过表达乳腺癌的大型随机试验正在进行中。与紫杉醇、芳香酶抑制剂或其他分子靶向药物的各种组合目前正在临床试验中进行研究。如果这些方法克服了曲妥珠单抗的局限性，拉帕替尼将在不久的将来成为乳腺癌的有效治疗选择。
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.