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奥拉帕利,卵巢癌的 PARP1 抑制剂。

Olaparib, PARP1 inhibitor in ovarian cancer.

机构信息

Sapienza University of Rome, Department of Gynecologic-Obstetrical and Urologic Sciences, Viale del Policlinico, 155 - 00161, Rome, Italy.

出版信息

Expert Opin Investig Drugs. 2012 Oct;21(10):1575-84. doi: 10.1517/13543784.2012.707189. Epub 2012 Jul 13.

Abstract

INTRODUCTION

Ovarian cancer is the most important cause of gynecological cancer-related mortality. Conventional treatments for advanced or recurrent disease offer limited results in terms of long-term responses and survival. Researches have recently focused on target therapies, which represent a new, promising, therapeutic approach, able to maximizing tumor kill and minimizing toxicity. The family of polyadenosine diphosphate-ribose polymerase (PARP) inhibitors is currently one of the most hopeful and investigated alternatives.

AREAS COVERED

Preclinical and clinical studies of Olaparib , the most investigated PARP inhibitor in ovarian cancer, are analyzed and discussed. Data were obtained by searching for all English peer-reviewed articles on Medline, on Cochrane Database and all on-going Phase I and II studies registered on National Cancer Institute Clinical Trials; also any related abstracts recently presented on Olaparib at major international congresses will be included.

EXPERT OPINION

Bad prognosis and drug resistance usually affect ovarian cancer. Recent trends toward the knowledge of molecular-specific pathways have produced new target drugs. PARP inhibition mediated by Olaparib in BRCA1 (breast cancer 1) and BRCA2 (breast cancer 2)-mutated and in sporadic ovarian cancer represents a promising field of investigation. Further studies are needed to confirm initial exciting results.

摘要

简介

卵巢癌是妇科癌症相关死亡的最重要原因。对于晚期或复发性疾病,传统治疗在长期反应和生存方面提供的效果有限。最近的研究集中在靶向治疗上,这是一种新的、有前途的治疗方法,能够最大限度地杀死肿瘤并最小化毒性。聚腺苷二磷酸核糖聚合酶(PARP)抑制剂家族目前是最有希望和研究最多的选择之一。

涵盖领域

对奥拉帕利(在卵巢癌中研究最多的 PARP 抑制剂)的临床前和临床研究进行了分析和讨论。通过在 Medline、Cochrane 数据库上搜索所有英语同行评议的文章,以及在国立癌症研究所临床试验上注册的所有 I 期和 II 期正在进行的研究,获得了数据;还将包括最近在主要国际大会上关于奥拉帕利的相关摘要。

专家意见

不良预后和耐药性通常会影响卵巢癌。最近对分子特异性途径的认识趋势产生了新的靶向药物。奥拉帕利介导的 PARP 抑制在 BRCA1(乳腺癌 1)和 BRCA2(乳腺癌 2)突变以及散发性卵巢癌中是一个有前途的研究领域。需要进一步的研究来证实最初令人兴奋的结果。

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