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Drug Evaluation

Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection

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Pages 97-103 | Published online: 20 Dec 2007

Keep up to date with the latest research on this topic with citation updates for this article.

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Lidija Kovač & Zdenko Časar. (2020) A literature review of the patent application publications on cabotegravir – an HIV integrase strand transfer inhibitor. Expert Opinion on Therapeutic Patents 30:3, pages 195-208.
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Qiu-Qin He, Xuan Zhang, Liu-Meng Yang, Yong-Tang Zheng & Fener Chen. (2013) Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 28:4, pages 671-676.
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Christine Katlama & Robert Murphy. (2009) Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection. Therapeutics and Clinical Risk Management 5, pages 331-340.
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Laura MacDonald, Mano Murty & Brian C Foster. (2009) Antiviral drug disposition and natural health products: risk of therapeutic alteration and resistance. Expert Opinion on Drug Metabolism & Toxicology 5:6, pages 563-578.
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C. Fenollar-Ferrer, V. Carnevale, S. Raugei & P. Carloni. (2008) HIV-1 integrase–DNA interactions investigated by molecular modelling. Computational and Mathematical Methods in Medicine 9:3-4, pages 231-243.
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Yue Wang, Shuang-Xi Gu, Qiuqin He & Renhua Fan. (2021) Advances in the development of HIV integrase strand transfer inhibitors. European Journal of Medicinal Chemistry 225, pages 113787.
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Nokuzola Mbhele, Benjamin Chimukangara & Michelle Gordon. (2021) HIV-1 integrase strand transfer inhibitors: a review of current drugs, recent advances and drug resistance. International Journal of Antimicrobial Agents 57:5, pages 106343.
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Leïla Belkhir, Carole Seguin-Devaux, Laure Elens, Caroline Pauly, Nicolas Gengler, Serge Schneider, Jean Ruelle, Vincent Haufroid & Bernard Vandercam. (2018) Impact of UGT1A1 polymorphisms on Raltegravir and its glucuronide plasma concentrations in a cohort of HIV-1 infected patients. Scientific Reports 8:1.
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Yue-Xia Bai, Long-Ji Li, Xiao-Li Wang, Cheng-Chu Zeng & Li-Ming Hu. (2014) Design and synthesis of N-hydroxytriazole-4-carboxamides as HIV integrase inhibitors. Medicinal Chemistry Research 24:1, pages 423-429.
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Wan-Gang Gu. (2014) Newly approved integrase inhibitors for clinical treatment of AIDS. Biomedicine & Pharmacotherapy 68:8, pages 917-921.
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Roberto Di Santo. (2013) Inhibiting the HIV Integration Process: Past, Present, and the Future. Journal of Medicinal Chemistry 57:3, pages 539-566.
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Vasanthanathan Poongavanam, N. S. Hari Narayana Moorthy & Jacob Kongsted. (2014) Dual mechanism of HIV-1 integrase and RNase H inhibition by diketo derivatives ? a computational study. RSC Adv. 4:73, pages 38672-38681.
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M. Van Loock, A. Hombrouck, T. Jacobs, B. Winters, G. Meersseman, K. Van Acker, R.F. Clayton & B.A. Malcolm. (2013) Reporter gene expression from LTR-circles as tool to identify HIV-1 integrase inhibitors. Journal of Virological Methods 187:2, pages 238-247.
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Serena Fortuna, Massimiliano Fabbiani, Simona Digiambenedetto, Enzo Ragazzoni, Lucia Lisi, Roberto Cauda & Pierluigi Navarra. (2013) Variability of Raltegravir Plasma Levels in the Clinical Setting. Pharmacology 92:1-2, pages 43-48.
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Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Metifiot, Steven J. Smith, B. Christie Vu, Christophe Marchand, Stephen H. Hughes, Yves Pommier & Terrence R. BurkeJrJr. (2012) Bicyclic Hydroxy-1H-pyrrolopyridine-trione Containing HIV-1 Integrase Inhibitors. Chemical Biology & Drug Design 79:2, pages 157-165.
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Antonio Piralla, Stefania Paolucci, Roberto Gulminetti, Giuditta Comolli & Fausto Baldanti. (2011) HIV integrase variability and genetic barrier in antiretroviral naïve and experienced patients. Virology Journal 8:1.
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Chenzhong Liao & Marc C. Nicklaus. 2011. HIV‐1 Integrase. HIV‐1 Integrase 429 455 .
Olivia Goethals, Marcia Van Ginderen, Ann Vos, Maxwell D. Cummings, Koen Van Der Borght, Liesbeth Van Wesenbeeck, Maxim Feyaerts, Ann Verheyen, Veerle Smits, Marnix Van Loock, Kurt Hertogs, Dominique Schols & Reginald F. Clayton. (2011) Resistance to raltegravir highlights integrase mutations at codon 148 in conferring cross-resistance to a second-generation HIV-1 integrase inhibitor. Antiviral Research 91:2, pages 167-176.
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Ted W. Johnson, Steven P. Tanis, Scott L. Butler, Deepak Dalvie, Dorothy M. DeLisle, Klaus R. Dress, Erik J. Flahive, Qiyue Hu, Jon E. Kuehler, Atsuo Kuki, Wen Liu, Guy A. McClellan, Qinghai Peng, Michael B. Plewe, Paul F. Richardson, Graham L. Smith, Jim Solowiej, Khanh T. Tran, Hai Wang, Xiaoming Yu, Junhu Zhang & Huichun Zhu. (2011) Design and Synthesis of Novel N -Hydroxy-Dihydronaphthyridinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors . Journal of Medicinal Chemistry 54:9, pages 3393-3417.
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Steven P. Tanis, Michael B. Plewe, Ted W. Johnson, Scott L. Butler, Deepak Dalvie, Dorothy DeLisle, Klaus R. Dress, Qiyue Hu, Buwen Huang, Jon E. Kuehler, Atsuo Kuki, Wen Liu, Qinghai Peng, Graham L. Smith, Jim Solowiej, Khanh T. Tran, Hai Wang, Anle Yang, Chunfeng Yin, Xiaoming Yu, Junhu Zhang & Huichun Zhu. (2010) Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK. Bioorganic & Medicinal Chemistry Letters 20:24, pages 7429-7434.
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Zixin Hu & Daniel R Kuritzkes. (2010) Effect of Raltegravir Resistance Mutations in HIV-1 Integrase on Viral Fitness. JAIDS Journal of Acquired Immune Deficiency Syndromes 55:2, pages 148-155.
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Donald J. AbrahamBrian A. Johns. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 75 106 .
James M. Smith, Allison Dauner, Bin Li, Priya Srinivasan, James Mitchell, Michael Hendry, Dennis Ellenberger, Sal Butera & Ron A. Otten. (2010) Generation of a dual RT Env SHIV that is infectious in rhesus macaques. Journal of Medical Primatology 39:4, pages 213-223.
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Chenzhong Liao, Christophe Marchand, Terrence R Burke Jr, Yves Pommier & Marc C Nicklaus. (2010) Authentic HIV-1 integrase inhibitors. Future Medicinal Chemistry 2:7, pages 1107-1122.
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Chenzhong Liao & Marc C Nicklaus. (2010) Computer tools in the discovery of HIV-1 integrase inhibitors. Future Medicinal Chemistry 2:7, pages 1123-1140.
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Olivia Goethals, Ann Vos, Marcia Van Ginderen, Peggy Geluykens, Veerle Smits, Dominique Schols, Kurt Hertogs & Reginald Clayton. (2010) Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to first-generation integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles. Virology 402:2, pages 338-346.
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Filippo Canducci, Maria Chiara Marinozzi, Michela Sampaolo, Enzo Boeri, Vincenzo Spagnuolo, Nicola Gianotti, Antonella Castagna, Stefania Paolucci, Fausto Baldanti, Adriano Lazzarin & Massimo Clementi. (2010) Genotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravir. Journal of Antimicrobial Chemotherapy 65:3, pages 425-433.
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Michael B. Plewe, Scott L. ButlerKlaus R. Dress, Qiyue Hu, Ted W. Johnson, Jon E. Kuehler, Atsuo Kuki, Hieu Lam, Wen Liu, Dawn Nowlin, Qinghai Peng, Sadayappan V. Rahavendran, Steven P. Tanis, Khanh T. Tran, Hai Wang, Anle Yang & Junhu Zhang. (2009) Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors. Journal of Medicinal Chemistry 52:22, pages 7211-7219.
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Christina Gavegnano & Raymond F Schinazi. (2009) Antiretroviral Therapy in Macrophages: Implication for HIV Eradication. Antiviral Chemistry and Chemotherapy 20:2, pages 63-78.
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Xue Zhi Zhao, Kasthuraiah Maddali, Christophe Marchand, Yves Pommier & Terrence R. BurkeJr.Jr.. (2009) Diketoacid-genre HIV-1 integrase inhibitors containing enantiomeric arylamide functionality. Bioorganic & Medicinal Chemistry 17:14, pages 5318-5324.
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Devendra K. Dhaked, Jitender Verma, Anil Saran & Evans C. Coutinho. (2008) Exploring the binding of HIV-1 integrase inhibitors by comparative residue interaction analysis (CoRIA). Journal of Molecular Modeling 15:3, pages 233-245.
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