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抗HIV新药raltegravir 被引量：1

A new antiretroviral agent against HIV:raltegravir
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摘要 整合酶(integrase)是HIV病毒复制的必需酶,因而成为抗HIV药物设计的一个合理靶点。目前尚无整合酶抑制剂类药物上市,raltegravir是第一个进入Ⅲ期临床的此类药物。与上市的抗HIV药物相比,具有更高或相近的抗逆转录病毒的活性,无交叉耐药性,毒副作用小,有可能成为第一个上市的整合酶抑制剂。现对其作用机制、临床前研究、药动学、临床应用及安全性等做一综述。 Integrase is essential for retroviral replication of human immunodeficiency virus and the rational target of the design of anti-HIV drug. To date, no IN inhibitor is approved by FDA for clinical use, rahegravir is the first one to enter into Phase III clinical trials. Compared with the anti-HIV drugs in the market, raltegravir is not only more or equal potent, but also no cross resistant, weak toxicity and side effect, et al. It may be the first approved integrase inhibitor for anti-HIV. This article reviews raltegravir in action mechanism, preclinical research ,clinical research, pharmacokinetic research and safety.
作者 谭艳梅 刘川 赵桂森
机构地区 山东大学药学院药物化学教研室
出处 《中国新药杂志》 CAS CSCD 北大核心 2007年第21期1812-1815,共4页 Chinese Journal of New Drugs
基金 国家自然科学基金(20472045)
关键词 抗HIV药 整合酶抑制剂 RALTEGRAVIR HIV integrase inhibitor raltegravir
分类号 R978.7 [医药卫生—药品]
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参考文献19

  • 1HAZUDA DJ,FELOCK P,WITMER M,et al.Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication incells[J].Science,2000,287(5453):646 -650.
  • 2Results from Two Phase Ⅲ Studies on ISENTRESSTM (raltegravir,MK-0518),Merck's Oral Investigational Integrase Inhibitor Presented at the Annual Conference on Retroviruses and Opportunistic infections(CROI)[EB/OL].(2006 -02 -09).http://www.merk.com/newsroom/press release/resea arch and development/html.
  • 3DAYAM R,DENG J,NEAMATI N.HIV-1 integrase inhibitors:2003-2004 update[J].Med Res Rev,2006,26 (3):271-309.
  • 4CHIU TK,DAVIES DR.Structure and function of HIV-1 integrase[J].Curr Top Med Chem,2004,4(9):965 -977.
  • 5ANTHONY NJ.HIV-1 Integrase:A target for new AIDS chemotherapeutics[J].Curr Top Med Chem,2004,4 (9):979 -990.
  • 6MILLER M,WITMER M,STILLMOCK K,et al.Biochemical and antiviral activity of MK-0518,a potent HIV integrase inhibitor[C]//16th Int AIDS Conf2006.Toronto:[s.n.],2006,Abst THPE0 302.
  • 7MILLER M,WITMER M,STILLMOCK K,et al.Biochemical and antiviral activity of MK-0518,a potent HIV integrane inhibitor[C]// 16th Int AIDS Conf 2006.Toronto:[s.n.],2006,AbstTHPE0 302.
  • 8PETRY AS,WENNING LA,LAETHEM M,et al.Safety,tolerability,and pharmacokinetics sfter single and multiple doses of MK-0518 in healthy subjects[C]//46th Intersci Conf Antimicrob Agents Chemother (ICAAC).San Francisco:[s.n.],2006,Abst A -3 76.
  • 9KASSAHUN K,MCINTOSH I,HRENIUK D,et al.Absorption,metabolism and excretion of MK-0518,a potent HIV-1 integrase inhibitor,in healthy male volunteers[C]//46th Intersci Conf Antimicrob Agents Chemother (ICAAC).San Francisco:[s.n.],2006,Abst A -372.
  • 10IWAMOTO M,WENNING LA,TROYER MD,et al.Lack of apharmacokinetic interaction of MK-0518 on midazolam (MDZ)[C]// 8th Int Congr Drug Ther HIV Infect 2006.Glasgow,:[s.n.],2006,Abst P300.

同被引文献15

  • 1毕毅,徐进宜,吴晓明.抗艾滋病药物的研究进展[J].中国现代应用药学,2005,22(6):461-465. 被引量：6
  • 2Strizki JM, Tremblay C, Xu S, et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1[J].Antimicrob Agents Chemother, 2005, 49 (12):4911.
  • 3Harris M, Montaner JS. Clinical uses of non-nucleoside reverse transcriptase inhibitors[J].Rev Med Viro, 2000, 10 (4):217.
  • 4Cvetkovic RS, Goa KL. Lopinavir/ritonavir: a review of its use in the management of HIV infection[J].Drugs, 2003,63 (8) : 769.
  • 5Sorberal A, Serradell N, Ros A, et al. Rilpivirine: reverse transcriptase inhibitor: anti-HIV agent[J]. Drugs Future, 2007,32 ( 12 ) : 1 046.
  • 6De Clercq E, Field HJ. Antiviral Chemistry & Chem otherapy' s current amiviral agents FactFile (2nd edition) : retroviruses and hepadnaviruses[J].Antivir Chem Chemother, 2008,19 (2) : 75.
  • 7Aruksakunwong O, Promsis K, Wittayanarakul K, et al. Current development on HIV-1 protease inhibitors[J]. Curr Pharm Des, 2007,3 (3) : 201.
  • 8Ysunila R, Susanl F, Maggiet A, et al. Safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus type 1 protease inhibitor, following repeat administration with and without ritonavir in healthy adult subjects[J].Antimicrob Agents Chemother , 2007, 51 (4) : 1 202.
  • 9Robert K, Mona P, Robert EW, et al.Synthesis, antiviral activity and pharmacokinetics of P1/P1' aubstituted 3- aminoindazole cyclic urea HIV protease inhibitors[J]. Bioorg Med Chem Lett , 2003,13 (6) : 605.
  • 10Kazuya S, Eiichi K, Yasuko S, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137 ) [J].J Virol, 2008,82 (2) : 764.

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中国新药杂志
2007年 第21期

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