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氟维司群在子宫内膜癌中的作用。

The role of fulvestrant in endometrial cancer.

机构信息

a Department of Obstetrics and Gynaecology , IRCCS-Fondazione Policlinico San Matteo, University of Pavia , Pavia , Italy.

b Department of Obstetrics and Gynaecology , IRCCS Azienda Ospedaliera Universitaria San Martino, IST Istituto Nazionale per la Ricerca sul Cancro, University of Genoa , Genoa , Italy.

出版信息

Expert Opin Drug Metab Toxicol. 2017 May;13(5):537-544. doi: 10.1080/17425255.2016.1244264. Epub 2016 Oct 19.

Abstract

Endometrial cancer is the most common malignancy of the female genital tract in industrialized countries. The traditional treatment of endometrial cancer is based on a surgical approach. In recent years, systemic endocrine therapy has demonstrated good efficacy in recurrent or metastatic setting, delaying progression, ameliorating quality of life and palliating symptoms. Areas covered: Phase I and II studies on selective estrogen receptor down-regulators used for the treatment of endometrial cancer treatment have been reviewed. The pharmacokinetic and pharmacodynamic features of selective receptor down-regulators have been also investigated. Expert opinion: Selective estrogen receptor down-regulators may exhibit clinical efficacy in the treatment of gynecological malignancies due to their pure estrogen receptor antagonist properties. However, up to now data are still limited and some unsolved questions remain. Fulvestrant has poor oral bioavailability and low pharmacodynamic characteristics. Further trials are required to examine new selective estrogen receptor down-regulator agents with better pharmacodynamic and pharmacokinetic profiles.

摘要

子宫内膜癌是工业化国家女性生殖道最常见的恶性肿瘤。子宫内膜癌的传统治疗方法基于手术。近年来,系统内分泌治疗在复发性或转移性疾病中显示出良好的疗效,可延缓疾病进展、改善生活质量和缓解症状。

涵盖领域

已对用于治疗子宫内膜癌的选择性雌激素受体下调剂的 I 期和 II 期研究进行了综述。还研究了选择性受体下调剂的药代动力学和药效学特征。

专家意见

由于选择性雌激素受体下调剂具有纯雌激素受体拮抗剂特性,因此可能在妇科恶性肿瘤的治疗中具有临床疗效。然而,到目前为止,数据仍然有限,仍存在一些悬而未决的问题。氟维司群口服生物利用度差,药效学特征低。需要进一步的试验来研究具有更好的药效学和药代动力学特征的新型选择性雌激素受体下调剂。

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