International Journal of Antimicrobial Agents
Volume 33, Issue 4 , Pages 307-320 , April 2009

Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV

Received 30 September 2008 ,Accepted 1 October 2008.

References 

  1. Barré-Sinoussi F, Chermann JC, Rey F, Nugeyre MT, Chamaret S, Gruest J, et al. Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS). Science. 1983;220:868–871
  2. Popovic M, Sarin PS, Robert-Gurroff M, Kalyanaraman VS, Mann D, Minowada J, et al. Isolation and transmission of human retrovirus (human T-cell leukemia virus). Science. 1983;219:856–859
  3. Mitsuya H, Popovic M, Yarchoan R, Matsushita S, Gallo RC, Broder S. Suramin protection of T cells in vitro against infectivity and cytopathic effect of HTLV-III. Science. 1984;226:172–174
  4. Broder S, Yarchoan R, Collins JM, Lane HC, Markham PD, Klecker RW, et al. Effects of suramin on HTLV-III/LAV infection presenting as Kaposi's sarcoma or AIDS-related complex: clinical pharmacology and suppression of virus replication in vivo. Lancet. 1985;2:627–630
  5. Mitsuya H, Weinhold KJ, Furman PA, St Clair MH, Lehrman SN, Gallo RC, et al. 3’-Azido-3’-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proc Natl Acad Sci U S A. 1985;82:7096–7100
  6. De Clercq E. Strategies in the design of antiviral drugs. Nat Rev Drug Discov. 2002;1:13–25
  7. De Clercq E. Anti-HIV drugs. Verh K Acad Geneesk Belg. 2007;64:81–104
  8. Tantillo C, Ding J, Jacobo-Molina A, Nanni RG, Boyer PL, Hughes SH, et al. Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Implications for mechanisms of drug inhibition and resistance. J Mol Biol. 1994;243:369–387
  9. Furman PA, Fyfe JA, St Clair MH, Weinhold K, Rideout JL, Freeman GA, et al. Phosphorylation of 3’-azido-3’-deoxythymidine and selective interaction of the 5’-triphosphate with human immunodeficiency virus reverse transcriptase. Proc Natl Acad Sci U S A. 1986;83:8333–8337
  10. Balzarini J, Holý A, Jindrich J, Naesens L, Snoeck R, Schols D, et al. Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine. Antimicrob Agents Chemother. 1993;37:332–338
  11. De Clercq E. Potential of acyclic nucleoside phosphonates in the treatment of DNA virus and retrovirus infections. Expert Rev Anti Infect Ther. 2003;1:21–43
  12. Baba M, Tanaka H, De Clercq E, Pauwels R, Balzarini J, Schols D, et al. Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. Biochem Biophys Res Commun. 1989;165:1375–1381
  13. Pauwels R, Andries K, Desmyter J, Schols D, Kukla MJ, Breslin HJ, et al. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature. 1990;343:470–474
  14. De Clercq E. Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future. Chem Biodivers. 2004;1:44–64
  15. Pauwels R. New non-nucleoside reverse transcriptase inhibitors (NNRTIs) in development for the treatment of HIV infections. Curr Opin Pharmacol. 2004;4:437–446
  16. Janssen PAJ, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, et al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem. 2005;48:1901–1909
  17. Pauwels R. Aspects of successful drug discovery and development. Antiviral Res. 2006;71:77–89
  18. Madruga JV, Cahn P, Grinsztejn B, Haubrich R, Lalezari J, Mills A, et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet. 2007;370:29–38
  19. Lazzarin A, Campbell T, Clotet B, Johnson M, Katlama C, Moll A, et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet. 2007;370:39–48
  20. Matthews T, Salgo M, Greenberg M, Chung J, DeMasi R, Bolognesi D. Enfuvirtide: the first therapy to inhibit the entry of HIV-1 into host CD4 lymphocytes. Nat Rev Drug Discov. 2004;3:215–225
  21. Westby M, van der Ryst E. CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection. Antivir Chem Chemother. 2005;16:339–354
  22. Perros M. CCR5 antagonists for the treatment of HIV infection and AIDS. Adv Antiviral Drug Design. 2007;5:185–212
  23. De Clercq E. The bicyclam AMD3100 story. Nat Rev Drug Discov. 2003;2:581–587
  24. Pommier Y, Johnson AA, Marchand C. Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov. 2005;4:236–248
  25. Grinsztejn B, Nguyen BY, Katlama C, Gatell JM, Lazzarin A, Vittecoq D, et al. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial. Lancet. 2007;369:1261–1269
  26. Steigbigel RT, Cooper DA, Kumar PN, Eron JE, Schechter M, Markowitz M, et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med. 2008;359:339–354
  27. Cooper DA, Steigbigel RT, Gatell JM, Rockstroh JK, Katlama C, Yeni P, et al. Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med. 2008;359:355–365
  28. Walensky RP, Paltiel AD, Losina E, Mercincavage LM, Schackman BR, Sax PE, et al. The survival benefits of AIDS treatment in the United States. J Infect Dis. 2006;194:11–19
  29. Hirsch MS. Entecavir surprise. N Engl J Med. 2007;356:2641–2643
  30. De Clercq E. The role of tenofovir in the prevention of HIV infections. AIDS. 2006;20:1990–1991
  31. Tsai CC, Follis KE, Sabo A, Beck TW, Grant RF, Bischofberger N, et al. Prevention of SIV infection in macaques by (R)-9-(2-phosphonylmethoxy-propyl)adenine. Science. 1996;270:1197–1199
  32. Otten RA, Smith DK, Adams DR, Pullium JK, Jackson E, Kim CN, et al. Efficacy of postexposure prophylaxis after intravaginal exposure of pig-tailed macaques to a human-derived retrovirus (human immunodeficiency virus type 2). J Virol. 2000;74:9771–9775
  33. Van Rompay KK, McChesney MB, Aguirre NL, Schmidt KA, Bischofberger N, Marthas ML. Two low doses of tenofovir protect newborn macaques against oral simian immunodeficiency virus infection. J Infect Dis. 2001;184:429–438

☆ Corresponds to lectures given at the International Conference ‘Drug Design and Discovery for Developing Countries’, International Centre for Science and High Technology (ICS), United Nations Industrial Development Organization (UNIDO), 3–5 July 2008, Trieste, Italy, and at The Fourteenth International Congress of Virology, 10–15 August 2008, Istanbul, Turkey.

PII: S0924-8579(08)00484-6

doi: 10.1016/j.ijantimicag.2008.10.010

International Journal of Antimicrobial Agents
Volume 33, Issue 4 , Pages 307-320 , April 2009

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