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Trastuzumab Emtansine: Mechanisms of Action and Resistance, Clinical Progress, and Beyond.
Trends in Cancer ( IF 14.3 ) Pub Date : 2020-01-21 , DOI: 10.1016/j.trecan.2019.12.010
Sara García-Alonso 1 , Alberto Ocaña 2 , Atanasio Pandiella 3
Affiliation  

The approval of ado-trastuzumab emtansine (T-DM1) for clinical use represented a turning point both in HER2-positive breast cancer treatment and antibody–drug conjugate (ADC) technology. T-DM1 has proved its value and effectiveness in advanced metastatic disease as well as in the adjuvant setting. However, its therapeutic potential extends beyond the treatment of breast cancer. Around 100 clinical trials have evaluated or are studying different aspects of T-DM1, such as its role in other HER2 malignancies, rational combinations with immunotherapy, or its function in brain metastasis. Conceptually, many lessons can be learned from this ADC. Understanding its mechanisms of action and the molecular basis underlying resistance to T-DM1 may be relevant to comprehend resistances raised to other ADCs and identify pitfalls that may be overcome.



中文翻译:

曲妥单抗Emtansine:作用和耐药机制,临床进展及其他。

ado-曲妥珠单抗Emtansine(T-DM1)在临床上的使用代表了HER2阳性乳腺癌治疗和抗体药物偶联(ADC)技术的转折点。T-DM1已证明其在晚期转移性疾病以及辅助治疗中的价值和有效性。但是,其治疗潜力超出了乳腺癌的治疗范围。大约100项临床试验已经评估或正在研究T-DM1的不同方面,例如其在其他HER2恶性肿瘤中的作用,与免疫疗法的合理组合或其在脑转移中的功能。从概念上讲,可以从此ADC中学到很多教训。了解其作用机理和对T-DM1的抗性的分子基础可能与理解对其他ADC的抗性并确定可以克服的陷阱有关。

更新日期:2020-01-21
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