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HER-dimerization inhibitors: evaluating pertuzumab in women's cancers.

机译：HER二聚体抑制剂：评估帕妥珠单抗在女性癌症中的作用。

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IMPORTANCE OF THE FIELD: Pertuzumab is a human EGF receptor (HER)-dimerization inhibitor that represent a novel class of agents aimed at blocking HER2 from pairing with other receptors of the HER family. In this review, we discuss the background and scientific rationale, related to pertuzumab as it has undergone development for women's cancers. AREAS COVERED IN THIS REVIEW: Pre-clinical and clinical trials, published or presented at national meetings from 1995 to the present, are included in this review. WHAT THE READER WILL GAIN: A Phase II trial in HER2-positive metastatic breast cancer showed promising activity of pertuzumab when it was combined with trastuzumab and a randomized Phase III trial is now underway. Pertuzumab, when evaluated in recurrent ovarian cancer showed limited activity when combined with chemotherapy in platinum-sensitive and platinum-resistant disease. However, a recent subset analysis suggests that HER3 mRNA levels may predict response to pertuzumab in ovarian cancer. TAKE HOME MESSAGE: HER-dimerization inhibitors represent a novel mechanism of inhibition of HER pathways. Pertuzumab may play a role in the management of HER2-positive breast cancer. The potential benefit of pertuzumab in ovarian cancer is unclear, but low HER3 levels may suggest a sub-group of patients that can benefit from pertuzumab.
机译：领域的重要性：帕妥珠单抗是人EGF受体（HER）-二聚化抑制剂，代表了旨在阻止HER2与HER家族其他受体配对的新型药物。在这篇综述中，我们讨论了与帕妥珠单抗有关的背景和科学原理，因为它已经发展成为可用于女性癌症的药物。该评价涵盖的领域：1995年至今在全国性会议上发表或介绍的临床前和临床试验均包括在本评价中。读者将获得什么：HER2阳性转移性乳腺癌的II期临床试验显示，当培妥珠单抗与曲妥珠单抗联合使用时，其有希望的活性，目前正在进行一项随机的III期试验。当在复发性卵巢癌中评估时，帕妥珠单抗与铂类敏感性和铂类抗性疾病的化学疗法联合使用时，其活性有限。但是，最近的子集分析表明，HER3 mRNA水平可能预测卵巢癌对帕妥珠单抗的反应。温馨提示：HER二聚化抑制剂代表了一种抑制HER途径的新机制。帕妥珠单抗可能在HER2阳性乳腺癌的治疗中发挥作用。帕妥珠单抗在卵巢癌中的潜在益处尚不清楚，但是较低的HER3水平可能表明可以从帕妥珠单抗中受益的亚组患者。

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