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新型非肽类蛋白酶抑制剂——地瑞那韦 被引量：1

A new nonpeptidic protease inhibitor——darunavir
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摘要 通过文献检索综述了地瑞那韦的药理作用、药动学特点、临床应用及安全性评价。地瑞那韦是新型非肽类蛋白酶抑制剂,临床上地瑞那韦与利托那韦合用,用于治疗曾经接受治疗的人免疫缺陷病毒(HIV)感染患者,本品对其他抗HIV治疗无效的患者具有较好的疗效及耐受性。 The aim is to introduce the pharmacology of darunavir.The pharmacokinetic parameters,clinical application and evaluation were reviewed from the newest published documents.As a new nonpeptidic protease inhibitor,darunavir combined with ritonavir（DRV/R） is approved for the treatment of antiretroviral therapy-experienced patients and was proved with good clinical efficacy and tolerance.
作者 郑宇静 张亚同 梁欣 傅得兴
机构地区 卫生部北京医院药学部 沈阳药科大学药学院
出处 《中国新药杂志》 CAS CSCD 北大核心 2009年第22期2131-2134,共4页 Chinese Journal of New Drugs
关键词 地瑞那韦 人免疫缺陷病毒 蛋白酶抑制剂 药理作用 临床评价 darunavir HIV protease inhibitor pharmacology clinical evaluation
分类号 R978.7 [医药卫生—药品]
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参考文献13

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  • 2VERMEIR M, LACHAU-DURAND S, MANNENS G,et al. Absorption, metabolism,and excretion of darunavir,a new protease inhibitor, administered alone and with low-dose ritonavir in healthy subjects [ J ]. Drug Metab Dispos, 2009,37 ( 4 ) : 809 - 820.
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同被引文献22

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  • 2Pauwels R. Mini-review: aspects of successful drug discovery and development[J]. Antivir Res, 2006, 71:77-89.
  • 3Martinez-Cajas JL, Wainberg MA. Protease inhibitor resistance in HIV infected patients: molecular and clinical perspectives. Antivir [J]. Res, 2007,76: 203-221.
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  • 5Ghosh AK, Dawson ZL, Mitsuya H. Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV [J]. Bioorg Med Chem, 2007, 15: 7576-7580.
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  • 8King NM, Prabu-jeyabalan M, Nalivai KA, et al. Structural and thermdynamic basis for the binding of TMCll4, an ext-generation human immunodeficiency virus typel protease inhibitor[J]. J Viol, 2004, 78(21): 12012-12021.
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  • 10Michael L, a-and 13-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors[P]. US: 6248775, 1998-06-19.

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中国新药杂志
2009年 第22期

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