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Adecatumumab: an anti-EpCAM monoclonal antibody, from the bench to the bedside.

机译:Adecatumumab:一种从长凳到床边的抗EpCAM单克隆抗体。

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IMPORTANCE OF THE FIELD: In developing new anticancer drugs, the identification of relevant targets is a key issue of growing importance. Ideally, an anticancer drug target should be specific to cancer cells, in order to both increase efficacy and decrease toxicity of the compound. AREAS COVERED IN THIS REVIEW: Epithelial cell adhesion molecule (EpCAM) is a membrane protein with proto-oncogenic properties that is expressed in a number of endothelium-derived cancers and is a promising anticancer drug target. Adecatumumab is a monoclonal, fully human IgG1 antibody that targets EpCAM, development of which is at present reaching Phase III trials. WHAT THE READER WILL GAIN: From a review of literature, we here update the rationale for using EpCAM as an anticancer target for monoclonal antibodies, with a special focus on adecatumumab. The fully human nature of adecatumumab is also discussed to put the drug in perspective with other related anti-EpCAM monoclonal antibodies, such as edrecolomab and catumaxomab. Adecatumumab studies are recapitulated, in order to provide the reader with a comprehensive view of the development of this promising anticancer agent. TAKE HOME MESSAGE: Adecatumumab is a promising fully human monoclonal antibody targeting EpCAM which is expressed in almost all adenocarcinomas and its activity is not dependent of K-Ras status.
机译:领域的重要性:在开发新的抗癌药物中,确定相关靶标是越来越重要的关键问题。理想地,抗癌药物靶标应对癌细胞具有特异性,以便既提高功效又降低化合物的毒性。综述中涉及的区域:上皮细胞粘附分子(EpCAM)是一种具有原癌性的膜蛋白,在许多内皮源性癌症中表达,并且是有希望的抗癌药物靶标。 Adecatumumab是靶向EpCAM的单克隆完整人类IgG1抗体,目前其开发已进入III期试验。读者的收获:从文献回顾中,我们在这里更新了将EpCAM用作单克隆抗体的抗癌靶标的原理,特别侧重于adecatumumab。还讨论了adecatumumab的完全人类本性,以便将该药物与其他相关的抗EpCAM单克隆抗体(例如edrecolomab和catumaxomab)结合使用。总结了Adecatumumab的研究,以便为读者提供这种有前途的抗癌药开发的全面视图。温馨提示:Adecatumumab是一种有针对性的针对人EpCAM的完全人单克隆抗体,该抗体在几乎所有腺癌中都有表达,其活性与K-Ras状态无关。

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