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Volumn 54, Issue 2, 2010, Pages 718-727

TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1

Author keywords

[No Author keywords available]

Indexed keywords

4 BENZOYL 1 [(4 METHOXY 1H PYRROLO[2,3 B]PYRIDIN 3 YL)OXOACETYL] 2 METHYLPIPERAZINE; ABACAVIR; AMPRENAVIR; ATAZANAVIR; DARUNAVIR; DIDANOSINE; EFAVIRENZ; EMIVIRINE; EMTRICITABINE; ENFUVIRTIDE; ETRAVIRINE; INDINAVIR; LAMIVUDINE; LOPINAVIR; MARAVIROC; NELFINAVIR; NEVIRAPINE; PLERIXAFOR; RALTEGRAVIR; RILPIVIRINE; RITONAVIR; SAQUINAVIR; STAVUDINE; TENOFOVIR; TIPRANAVIR; ZALCITABINE; ZIDOVUDINE;

EID: 75749118495     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00986-09     Document Type: Article
Times cited : (265)

References (52)
  • 6
    • 20144370682 scopus 로고    scopus 로고
    • Benjahad, A., M. Croisy, C. Monneret, E. Bisagni, D. Mabire, S. Coupa, A. Poncelet, I. Csoka, J. Guillemont, C. Meyer, K. Andries, R. Pauwels, M. P. de Béthune, D. M. Himmel, K. Das, E. Arnold, C. H. Nguyen, and D. S. Grierson. 2005. 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)- ones: in vitro evaluation of new C-3-amino-subsituted and C-5,6-alkyl- substituted analogues against clinically important HIV mutant strains. J. Med. Chem. 48:1948-1964.
    • Benjahad, A., M. Croisy, C. Monneret, E. Bisagni, D. Mabire, S. Coupa, A. Poncelet, I. Csoka, J. Guillemont, C. Meyer, K. Andries, R. Pauwels, M. P. de Béthune, D. M. Himmel, K. Das, E. Arnold, C. H. Nguyen, and D. S. Grierson. 2005. 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)- ones: in vitro evaluation of new C-3-amino-subsituted and C-5,6-alkyl- substituted analogues against clinically important HIV mutant strains. J. Med. Chem. 48:1948-1964.
  • 7
    • 0024847290 scopus 로고
    • What is synergy?
    • Berenbaum, M. C. 1989. What is synergy? Pharmacol. Rev. 41:93-141.
    • (1989) Pharmacol. Rev , vol.41 , pp. 93-141
    • Berenbaum, M.C.1
  • 8
    • 0029891663 scopus 로고    scopus 로고
    • Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease
    • Bilello, J. A., P. A. Bilello, K. Stellrecht, J. Leonard, D. W. Norbeck, D. J. Kempf, T. Robins, and G. L. Drusano. 1996. Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob. Agents Chemother. 40:1491-1497.
    • (1996) Antimicrob. Agents Chemother , vol.40 , pp. 1491-1497
    • Bilello, J.A.1    Bilello, P.A.2    Stellrecht, K.3    Leonard, J.4    Norbeck, D.W.5    Kempf, D.J.6    Robins, T.7    Drusano, G.L.8
  • 9
    • 0028919933 scopus 로고
    • The inhibition of human immunodeficiency virus type 1 in vitro by a non-nucleoside reverse transcriptase inhibitor MKC-442, alone and in combination with other anti-HIV compounds
    • Brennan, T. M., D. L. Taylor, C. G. Bridges, J. P. Leyda, and A. S. Tyms. 1995. The inhibition of human immunodeficiency virus type 1 in vitro by a non-nucleoside reverse transcriptase inhibitor MKC-442, alone and in combination with other anti-HIV compounds. Antiviral Res. 26:173-187.
    • (1995) Antiviral Res , vol.26 , pp. 173-187
    • Brennan, T.M.1    Taylor, D.L.2    Bridges, C.G.3    Leyda, J.P.4    Tyms, A.S.5
  • 10
    • 0025810128 scopus 로고
    • Characterization of an HIV-1 isolate displaying an apparent absence of virion-associated reverse transcriptase activity
    • Buckheit, R. W., Jr., and R. Swanstrom. 1991. Characterization of an HIV-1 isolate displaying an apparent absence of virion-associated reverse transcriptase activity. AIDS Res. Hum. Retroviruses 7:295-302.
    • (1991) AIDS Res. Hum. Retroviruses , vol.7 , pp. 295-302
    • Buckheit Jr., R.W.1    Swanstrom, R.2
  • 11
    • 0027967566 scopus 로고
    • Potent and specific inhibition of HIV envelope-mediated cell fusion and virus binding by G quartet-forming oligonucleotide (ISIS 5320)
    • Buckheit, R. W., Jr., J. L. Roberson, C. Lackman-Smith, J. R. Wyatt, T. A. Vickers, and D. J. Ecker. 1994. Potent and specific inhibition of HIV envelope-mediated cell fusion and virus binding by G quartet-forming oligonucleotide (ISIS 5320). AIDS Res. Hum. Retroviruses 10:1497-1506.
    • (1994) AIDS Res. Hum. Retroviruses , vol.10 , pp. 1497-1506
    • Buckheit Jr., R.W.1    Roberson, J.L.2    Lackman-Smith, C.3    Wyatt, J.R.4    Vickers, T.A.5    Ecker, D.J.6
  • 12
    • 0028227096 scopus 로고
    • Structure of serum albumin
    • Carter, D. C., and J. X. Ho. 1994. Structure of serum albumin. Adv. Protein Chem. 45:153-203.
    • (1994) Adv. Protein Chem , vol.45 , pp. 153-203
    • Carter, D.C.1    Ho, J.X.2
  • 13
    • 0021118703 scopus 로고
    • Quantitative analysis of dose-effect relationships: The combined effects of multiple drugs or enzyme inhibitors
    • Chou, T. C., and P. Talalay. 1984. Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv. Enzyme Regul. 22:27-55.
    • (1984) Adv. Enzyme Regul , vol.22 , pp. 27-55
    • Chou, T.C.1    Talalay, P.2
  • 14
    • 0000885268 scopus 로고    scopus 로고
    • Scintillation proximity assay-a versatile high throughput screening technology
    • Cook, N. D. 1996. Scintillation proximity assay-a versatile high throughput screening technology. Drug Discov. Today 1:287-294.
    • (1996) Drug Discov. Today , vol.1 , pp. 287-294
    • Cook, N.D.1
  • 15
    • 40349091258 scopus 로고    scopus 로고
    • High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: Strategic flexibility explains potency against resistance mutations
    • Das, K., J. B. Bauman, A. D. Clark, Jr., Y. V. Frenkel, P. J. Lewi, A. J. Shatkin, S. H. Hughes, and E. Arnold. 2008. High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations. Proc. Natl. Acad. Sci. U. S. A. 105:1466-1471.
    • (2008) Proc. Natl. Acad. Sci. U. S. A , vol.105 , pp. 1466-1471
    • Das, K.1    Bauman, J.B.2    Clark Jr., A.D.3    Frenkel, Y.V.4    Lewi, P.J.5    Shatkin, A.J.6    Hughes, S.H.7    Arnold, E.8
  • 18
    • 0034786988 scopus 로고    scopus 로고
    • Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen
    • Delaugerre, C., R. Rohban, A. Simon, M. Mouroux, C. Tricot, R. Agher, J. M. Huraux, C. Katlama, and V. Calvez. 2001. Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J. Med. Virol. 65:445-448.
    • (2001) J. Med. Virol , vol.65 , pp. 445-448
    • Delaugerre, C.1    Rohban, R.2    Simon, A.3    Mouroux, M.4    Tricot, C.5    Agher, R.6    Huraux, J.M.7    Katlama, C.8    Calvez, V.9
  • 20
    • 40349094606 scopus 로고    scopus 로고
    • Two-dimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase
    • Fang, C., J. D. Bauman, K. Das, A. Remorino, E. Arnold, and R. M. Hochstrasser. 2008. Two-dimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase. Proc. Natl. Acad. Sci. U. S. A. 105:1472-1477.
    • (2008) Proc. Natl. Acad. Sci. U. S. A , vol.105 , pp. 1472-1477
    • Fang, C.1    Bauman, J.D.2    Das, K.3    Remorino, A.4    Arnold, E.5    Hochstrasser, R.M.6
  • 23
    • 0344474694 scopus 로고    scopus 로고
    • Hertogs, K., M. P. de Béthune, V. Miller, T. Ivens, P. Schel, A. Van Cauwenberge, C. Van Den Eynde, V. Van Gerwen, H. Azijn, M. Van Houtte, F. Peeters, S. Staszewski, M. Conant, S. Bloor, S. Kemp, B. Larder, and R. Pauwels. 1998. A rapid method for simultaneous detection of phenotypic resistance to inhibitors of protease and reverse transcriptase in recombinant human immunodeficiency virus type 1 isolates from patients treated with antiretroviral drugs. Antimicrob. Agents Chemother. 42:269-276.
    • Hertogs, K., M. P. de Béthune, V. Miller, T. Ivens, P. Schel, A. Van Cauwenberge, C. Van Den Eynde, V. Van Gerwen, H. Azijn, M. Van Houtte, F. Peeters, S. Staszewski, M. Conant, S. Bloor, S. Kemp, B. Larder, and R. Pauwels. 1998. A rapid method for simultaneous detection of phenotypic resistance to inhibitors of protease and reverse transcriptase in recombinant human immunodeficiency virus type 1 isolates from patients treated with antiretroviral drugs. Antimicrob. Agents Chemother. 42:269-276.
  • 24
    • 75749092061 scopus 로고    scopus 로고
    • Jakubik, J. J., C. Chapron, L. Hubbard, M. Seifer, and D. N. Standring. 2008. In vitro cross-resistance profile for a next-generation NNRTI: IDX899, poster 26. Abstr. XVII Int. HIV Drug Resist. Workshop.
    • Jakubik, J. J., C. Chapron, L. Hubbard, M. Seifer, and D. N. Standring. 2008. In vitro cross-resistance profile for a next-generation NNRTI: IDX899, poster 26. Abstr. XVII Int. HIV Drug Resist. Workshop.
  • 25
    • 20144372481 scopus 로고    scopus 로고
    • Janssen, P. A., P. J. Lewi, E. Arnold, F. Daeyaert, M. de Jonge, J. Heeres, L. Koymans, M. Vinkers, J. Guillemont, E. Pasquier, M. Kukla, D. Ludovici, K. Andries, M.-P. de Béthune, R. Pauwels, K. Das, A. D. Clark, Jr., Y. V. Frenkel, S. H. Hughes, B. Medaer, F. De Knaep, H. Bohets, F. De Clerck, A. Lampo, P. Williams, and P. Stoffels. 2005. 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. 48:1901-1909.
    • Janssen, P. A., P. J. Lewi, E. Arnold, F. Daeyaert, M. de Jonge, J. Heeres, L. Koymans, M. Vinkers, J. Guillemont, E. Pasquier, M. Kukla, D. Ludovici, K. Andries, M.-P. de Béthune, R. Pauwels, K. Das, A. D. Clark, Jr., Y. V. Frenkel, S. H. Hughes, B. Medaer, F. De Knaep, H. Bohets, F. De Clerck, A. Lampo, P. Williams, and P. Stoffels. 2005. 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. 48:1901-1909.
  • 26
    • 1542526970 scopus 로고
    • Nigrosin as a dye for differentiating live and dead ascites cells
    • Kaltenbach, J. P., M. H. Kaltenbach, and W. B. Lyons. 1958. Nigrosin as a dye for differentiating live and dead ascites cells. Exp. Cell Res. 15:112-117.
    • (1958) Exp. Cell Res , vol.15 , pp. 112-117
    • Kaltenbach, J.P.1    Kaltenbach, M.H.2    Lyons, W.B.3
  • 27
    • 0027916595 scopus 로고
    • Quantitative detection of HIV-1 drug resistance mutations by automated DNA sequencing
    • Larder, B. A., A. Kohli, P. Kellam, S. D. Kemp, M. Kronick, and R. D. Henfrey. 1993. Quantitative detection of HIV-1 drug resistance mutations by automated DNA sequencing. Nature 365:671-673.
    • (1993) Nature , vol.365 , pp. 671-673
    • Larder, B.A.1    Kohli, A.2    Kellam, P.3    Kemp, S.D.4    Kronick, M.5    Henfrey, R.D.6
  • 28
    • 75749105247 scopus 로고    scopus 로고
    • Establishment of biological cut-off values for predicting resistance to therapy
    • November, U.S. patent 7,292,944
    • Larder, B., R. P. Harrigan, and K. Hertogs. November 2007. Establishment of biological cut-off values for predicting resistance to therapy. U.S. patent 7,292,944.
    • (2007)
    • Larder, B.1    Harrigan, R.P.2    Hertogs, K.3
  • 32
    • 75749089116 scopus 로고    scopus 로고
    • The safety and efficacy of tenofovir DF (TDF) in combination with lamivudine (3TC) and efavirenz (EFV) in antiretroviralnaïve patients through seven years
    • poster P004, Cong. Drug Ther. HIV Infect
    • Madruga, J. V. R., I. Cassetti, A. Etzel, J. Suleiman, Y. Zhou, A. K. Cheng, and J. Enejosa. 2008. The safety and efficacy of tenofovir DF (TDF) in combination with lamivudine (3TC) and efavirenz (EFV) in antiretroviralnaïve patients through seven years, poster P004. Abstr. 9th Int. Cong. Drug Ther. HIV Infect.
    • (2008) Abstr. 9th Int
    • Madruga, J.V.R.1    Cassetti, I.2    Etzel, A.3    Suleiman, J.4    Zhou, Y.5    Cheng, A.K.6    Enejosa, J.7
  • 34
    • 0027310686 scopus 로고
    • Alpha 1-acid glycoprotein levels in AIDS patients before and after short-term treatment with zidovudine (ZDV)
    • Oie, S., M. A. Jacobson, and D. I. Abrams. 1993. Alpha 1-acid glycoprotein levels in AIDS patients before and after short-term treatment with zidovudine (ZDV). J. Acquir. Immune Defic. Syndr. 6:531-533.
    • (1993) J. Acquir. Immune Defic. Syndr , vol.6 , pp. 531-533
    • Oie, S.1    Jacobson, M.A.2    Abrams, D.I.3
  • 37
    • 0037221414 scopus 로고    scopus 로고
    • Travel and the spread of HIV-1 genetic variants
    • Perrin, L., L. Kaiser, and S. Yerly. 2003. Travel and the spread of HIV-1 genetic variants. Lancet Infect. Dis. 3:22-27.
    • (2003) Lancet Infect. Dis , vol.3 , pp. 22-27
    • Perrin, L.1    Kaiser, L.2    Yerly, S.3
  • 38
    • 73649148381 scopus 로고    scopus 로고
    • Pozniak, A. L., J. Morales-Ramirez, E. Katabira, D. Steyn, S. H. Lupo, M. Santoscoy, B. Grinsztejn, K. Ruxrungtham, L. T. Rimsky, S. Vanveggel, and K. Boven. 2010. Efficacy and safety of TMC278 in antiretroviral-naïve HIV-1 patients: week 96 results of a phase IIb randomized trial. AIDS 24:55-65.
    • Pozniak, A. L., J. Morales-Ramirez, E. Katabira, D. Steyn, S. H. Lupo, M. Santoscoy, B. Grinsztejn, K. Ruxrungtham, L. T. Rimsky, S. Vanveggel, and K. Boven. 2010. Efficacy and safety of TMC278 in antiretroviral-naïve HIV-1 patients: week 96 results of a phase IIb randomized trial. AIDS 24:55-65.
  • 39
    • 75749097137 scopus 로고    scopus 로고
    • Pozniak, A., J. Morales-Ramirez, L. Mohapi, M. Santoscoy, P. Chetchotisakd, M. Hereygers, S. Vanveggel, M. Peeters, B. Woodfall, and K. Boven. 2007. 48-week primary analysis of trial TMC278-C204: TMC278 demonstrates potent and sustained efficacy in ART naive patients, abstr. 144 LB. Abstr. 14th Conf. Retroviruses Opportunistic Infect.
    • Pozniak, A., J. Morales-Ramirez, L. Mohapi, M. Santoscoy, P. Chetchotisakd, M. Hereygers, S. Vanveggel, M. Peeters, B. Woodfall, and K. Boven. 2007. 48-week primary analysis of trial TMC278-C204: TMC278 demonstrates potent and sustained efficacy in ART naive patients, abstr. 144 LB. Abstr. 14th Conf. Retroviruses Opportunistic Infect.
  • 40
    • 0024993530 scopus 로고    scopus 로고
    • Prichard, M. N., and C. Shipman, Jr. 1990. A three-dimensional model to analyze drug-drug interactions. Antiviral Res. 14:181-205.
    • Prichard, M. N., and C. Shipman, Jr. 1990. A three-dimensional model to analyze drug-drug interactions. Antiviral Res. 14:181-205.
  • 43
    • 1642535388 scopus 로고    scopus 로고
    • Molecular mechanism of a AMD3100 antagonism in the CXCR4 receptor transfer of binding site to the CXCR3 receptor
    • Rosenkilde, M. M., L.-O. Gerlach, J. S. Jakobsen, R. T. Skerlj, G. J. Bridger, and T. W. Schwartz. 2004. Molecular mechanism of a AMD3100 antagonism in the CXCR4 receptor transfer of binding site to the CXCR3 receptor. J. Biol. Chem. 279:3033-3041.
    • (2004) J. Biol. Chem , vol.279 , pp. 3033-3041
    • Rosenkilde, M.M.1    Gerlach, L.-O.2    Jakobsen, J.S.3    Skerlj, R.T.4    Bridger, G.J.5    Schwartz, T.W.6
  • 44
    • 0019887799 scopus 로고
    • Identification of common molecular subsequences
    • Smith, T. F., and M. S. Waterman. 1981. Identification of common molecular subsequences. J. Mol. Biol. 147:195-197.
    • (1981) J. Mol. Biol , vol.147 , pp. 195-197
    • Smith, T.F.1    Waterman, M.S.2
  • 45
    • 46749104685 scopus 로고    scopus 로고
    • Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: The development pipeline and recent clinical data
    • Sweeney, Z. K., and K. Klumpp. 2008. Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: the development pipeline and recent clinical data. Curr. Opin. Drug Discov. Devel. 11:458-470.
    • (2008) Curr. Opin. Drug Discov. Devel , vol.11 , pp. 458-470
    • Sweeney, Z.K.1    Klumpp, K.2
  • 47
    • 75749096484 scopus 로고    scopus 로고
    • Tibotec Pharmaceuticals, Ltd. 2008. Intelence product information. Tibotec Pharmaceuticals, Ltd., Mechelen, Belgium. http://www.intelence-info.com /intelence/assets/pdf/INTELENCE-PI.pdf.
    • Tibotec Pharmaceuticals, Ltd. 2008. Intelence product information. Tibotec Pharmaceuticals, Ltd., Mechelen, Belgium. http://www.intelence-info.com /intelence/assets/pdf/INTELENCE-PI.pdf.
  • 48
    • 34547841291 scopus 로고    scopus 로고
    • Vermeiren, H., E. Van Craenenbroeck, P. Alen, L. Bacheler, G. Picchio, P. Lecocq, and the Virco Clinical Response Collaborative Team. 2007. Prediction of HIV-1 drug susceptibility phenotype from the viral genotype using linear regression modeling. J. Virol. Methods 145:47-55.
    • Vermeiren, H., E. Van Craenenbroeck, P. Alen, L. Bacheler, G. Picchio, P. Lecocq, and the Virco Clinical Response Collaborative Team. 2007. Prediction of HIV-1 drug susceptibility phenotype from the viral genotype using linear regression modeling. J. Virol. Methods 145:47-55.
  • 50
    • 75749150723 scopus 로고    scopus 로고
    • Antivirogram phenotype report
    • Belgium
    • Virco. 2009. Antivirogram phenotype report. Virco BVBA, Mechelen, Belgium. http://www.vircolab.com/product-center/antivirogram/the-antivirogram- report.
    • (2009) Virco BVBA, Mechelen
    • Virco1
  • 51
    • 75749090639 scopus 로고    scopus 로고
    • The virco® TYPE HIV-1 report
    • Belgium
    • Vircolab. 2009. The virco® TYPE HIV-1 report. Virco BVBA, Mechelen, Belgium. http://www.vircolab.com/product-center/vircotype-hiv-1/the- vircotype-hiv-1-report.
    • (2009) Virco BVBA, Mechelen
  • 52
    • 2942704146 scopus 로고    scopus 로고
    • Clinical utility of current NNRTIs and perspectives of new agents in this class under development
    • Zhang, Z., R. Hamatake, and Z. Hong. 2004. Clinical utility of current NNRTIs and perspectives of new agents in this class under development. Antivir. Chem. Chemother. 15:121-134.
    • (2004) Antivir. Chem. Chemother , vol.15 , pp. 121-134
    • Zhang, Z.1    Hamatake, R.2    Hong, Z.3


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