摘要
了解去势耐药前列腺癌的耐药机制。 背景:左旋脲(MDV 3100,XTANDI)是第二代雄激素受体抑制剂,专为治疗去势耐药前列腺癌(Crpc)而设计,具有较长的生存期。是时候了。MDV 3100耐药的机制尚不清楚,大多数接受治疗的患者,无论是先天的还是后天的,都会出现耐药性。 目的:本综述旨在总结MDV3100抗性机制中可用的主要数据。 了解所引起的阻力对und具有临床意义在日常实践和改进策略中,对预后和预测生物标志物的有效性进行了评价。 结果:MDV 3100的耐药主要可分为两种不同的途径,一是依赖于雄激素受体的活性,二是与雄激素受体的活性无关。雄激素受体(AR)轴位于第一位。前列腺癌细胞的重要通路,目前仍被认为是一种重要的耐药机制。 结论:靶向这些新识别的信号,尤其是AR轴,可能通过新的治疗剂潜在地克服,协同地改善CRPC中的ADT。
关键词: 去势抵抗性前列腺癌,enzalutamide,耐药性,雄激素受体,生物标志物,抑制剂。
图形摘要
Current Drug Targets
Title:Drug Resistance of Enzalutamide in CRPC
Volume: 19 Issue: 6
关键词: 去势抵抗性前列腺癌,enzalutamide,耐药性,雄激素受体,生物标志物,抑制剂。
摘要: Understanding and targeting the mechanisms of resistance to enzalutamide in castration resistant prostate cancer.
Background: Enzalutamide (MDV3100, XTANDI) is a second generation androgen receptor inhibitor that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged survival time. The mechanisms of mdv3100 resistance have not yet been clearly clarified and the majority of treated patients, innate or acquiring resistance invariably arises.
Objective: The purpose of this review is to summarize the main data available on the mechanisms of resistance to mdv3100. Understanding how the resistance aroused may have clinical implications in underlying the usefulness of prognostic and predictive biomarkers in daily practice and improving the strategies.
Results: Resistance to MDV3100 could be basically divided into two distinct pathways, either dependent or independent of the androgen receptor activity. Androgen receptor (AR) axis is sitll the most important pathway for prostate cancer cells and it is still currently regarded as a critical resistant mechanism.
Conclusion: Targeting these newly identified signals, especially AR axis, could be potentially overcome through novel therapeutic agents, synergically improve the ADT in CRPC.
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Cite this article as:
Drug Resistance of Enzalutamide in CRPC, Current Drug Targets 2018; 19 (6) . https://dx.doi.org/10.2174/1389450118666170417144250
DOI https://dx.doi.org/10.2174/1389450118666170417144250 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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