[關(guān)鍵詞]
[摘要]
研究發(fā)現(xiàn),雄激素受體與前列腺癌的發(fā)生存在密切關(guān)系。雄激素拮抗療法成為臨床治療早期前列腺癌的有效手段,近20年來(lái)已有多個(gè)藥物上市(如氟他胺、羥基氟他胺和比卡魯胺等),但這些經(jīng)典的藥物在治療中易產(chǎn)生抗雄激素撤除綜合癥等問(wèn)題,因此其應(yīng)用受到限制。目前,新近研發(fā)的非甾體類雄激素受體拮抗劑(如RD162、MDV3100和BMS-641988)活性更強(qiáng),正進(jìn)行臨床試驗(yàn),并有望解決過(guò)去雄激素受體拮抗劑存在的問(wèn)題。查閱國(guó)內(nèi)外相關(guān)文獻(xiàn),對(duì)已上市藥物、當(dāng)前臨床研究的藥物以及近年發(fā)現(xiàn)的小分子雄激素受體抑制劑的研究進(jìn)展進(jìn)行綜述。
[Key word]
[Abstract]
The study has found that androgen receptor is closely associated with development of prostate cancer, and now, androgen antagonist therapy has become an effective way of clinical treatment for early prostate cancer. A number of drugs were launched in the past two decades such as flutamide, hydroxyl-flutamide, and bicalutamide. However, these classic drugs were easy in the anti-androgen withdrawal syndrome which limited their application in clinical. At present, the newly-developed non-steroidal androgen receptor antagonists (such as RD162, MDV3100, and BMS-641988) show more potent activity and are tested in clinical trials, which could solve the above problems to some extents. This paper summarizes the progress on the launched drugs, the current clinical studied drugs and small-molecule androgen receptor antagonists based on relevant literatures.
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