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首页> 外文期刊>Expert opinion on biological therapy >Trastuzumab emtansine in breast cancer.
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Trastuzumab emtansine in breast cancer.

机译：曲妥珠单抗Emtansine在乳腺癌中的作用。

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摘要

Trastuzumab emtansine (T-DM1) is a human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) composed of trastuzumab, a stable linker (MCC), and the cytotoxic agent DM1 (derivative of maytansine). Administration of T-DM1 leads to limited systemic exposure of free DM1, with no evidence of DM1 accumulation after repeated dosing. AREAS COVERED: Phase I and Phase II clinical trials with T-DM1 as a single agent and in combination with paclitaxel, docetaxel, and pertuzumab have shown substantial clinical activity and a favorable safety profile. A randomized, open-label, first-line trial comparing trastuzumab and docetaxel with single agent T-DM1 showed a significant improved progression-free survival for T-DM1. EXPERT OPINION: T-DM1 has successfully completed second-line Phase III development for advanced HER2-positive breast cancer. The Phase III EMILIA study demonstrated an overall survival benefit for T-DM1 compared to the combination of lapatinib and capecitabine in taxane-trastuzumab pretreated patients. T-DM1 may offer delivery on a personalized basis of very potent cytotoxic agents in a cellular selective manner.
机译：曲妥珠单抗Emtansine（T-DM1）是靶向人表皮生长因子受体2（HER2）的抗体-药物偶联物（ADC），由曲妥珠单抗，稳定的连接子（MCC）和细胞毒剂DM1（美登素的衍生物）组成。 T-DM1的给药导致游离DM1的全身暴露受限，在重复给药后没有DM1积累的迹象。覆盖的区域：以T-DM1为单一药物并与紫杉醇，多西紫杉醇和帕妥珠单抗联合使用的I期和II期临床试验已显示出显着的临床活性和良好的安全性。一项比较曲妥珠单抗和多西他赛与单一药物T-DM1的随机，开放标签，一线试验显示，T-DM1的无进展生存期显着改善。专家意见：T-DM1已成功完成针对晚期HER2阳性乳腺癌的二线III期开发。 EMILIA III期研究显示，在紫杉烷-曲妥珠单抗预处理的患者中，与拉帕替尼和卡培他滨组合相比，T-DM1的总体生存获益。 T-DM1可以以个性化的方式以细胞选择性方式提供非常有效的细胞毒剂。

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