Promising molecular targeted therapies in breast cancer.
Promising molecular targeted therapies in breast cancer.
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DOI：
10.4103/0253-7613.81497
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发表时间：
2011-05
影响因子：
2.4
通讯作者：
Gupta RC
中科院分区：
文献类型：
--
作者：
Munagala R;Aqil F;Gupta RC
近年来，人们对乳腺癌分子事件和关键通路的理解有了显着的进步。这导致了新靶标的确定和被称为靶向治疗的抗癌疗法的开发。靶向治疗对参与关键分子事件的分子具有高度特异性，这些事件负责癌症表型，例如细胞生长、存活、迁移、侵袭、转移、凋亡、细胞周期进展和血管生成。已批准用于乳腺癌的靶向药物包括针对人表皮生长因子受体2（HER2）的曲妥珠单抗和拉帕替尼以及针对血管内皮生长因子（VEGF）的贝伐单抗。目前正在临床前和临床试验中评估的其他几种靶向药物包括表皮生长因子受体（EGFR）抑制剂、EGFR和HER2双重抑制剂、VEGF/VEGFR抑制剂以及干扰PI3K/AKT/mTOR和RAS/MEK/ERK等关键信号通路的药物；抗其他酪氨酸激酶的药物，例如 Src、胰岛素样生长因子 (IGF)/IGF 受体 (IGFR)；促进细胞凋亡的药物，例如聚ADP核糖聚合酶抑制剂；针对侵袭和转移的药物，例如基质金属蛋白酶抑制剂等。在这篇综述中，我们重点介绍了临床试验中最有前途的靶向药物及其与主流化疗药物的组合。
In recent years, there has been a significant improvement in the understanding of molecular events and critical pathways involved in breast cancer. This has led to the identification of novel targets and development of anticancer therapies referred to as targeted therapy. Targeted therapy has high specificity for the molecules involved in key molecular events that are responsible for cancer phenotype such as cell growth, survival, migration, invasion, metastasis, apoptosis, cell-cycle progression, and angiogenesis. Targeted agents that have been approved for breast cancer include trastuzumab and lapatinib, directed against human epidermal growth factor receptor 2 (HER2) and bevacizumab, directed against vascular endothelial growth factor (VEGF). Several other targeted agents currently under evaluation in preclinical and clinical trials include inhibitors of epidermal growth factor receptor (EGFR), dual EGFR and HER2 inhibitors, VEGF/VEGFR inhibitors, and agents that interfere with crucial signaling pathways such as PI3K/AKT/mTOR and RAS/MEK/ERK; agents against other tyrosine kinases such as Src, insulin-like growth factor (IGF)/IGF-receptor (IGFR); agents that promote apoptosis such as Poly ADP ribose polymerase inhibitors; agents that target invasion and metastasis such as matrix metalloproteinases inhibitors and others. In this review, we highlight the most promising targeted agents and their combination with mainstream chemotherapeutic drugs in clinical trials.