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Enfuvirtide Resistance

T-1249 demonstrated substantial activity against enfuvirtide-resistant viruses in clinical studies (Melby et al. 2007a) however, development was discontinued due to formulation issues. Additional peptides with more potent activity were subsequently designed, which also showed much improved pharmacokinetic properties (Dwyer et al. 2007) however, the availability of oral agents in other new classes makes the likelihood of the development of these agents uncertain. [Pg.186]

Labrosse B, Morand-Joubert L, Goubard A, Rochas S, Labemardiere JL, Pacanowski J, Meynard JL, Hance AJ, Clavel E, Mammano E (2006) Role of the envelope genetic context in the development of enfuvirtide resistance in human immunodeficiency virus type 1-infected patients. J Virol 80 8807-8819... [Pg.197]

Melby T, DeMasi R, MiraUes G, HeUek-Snyder G, Greenberg M (2005) Evolution of enfuvirtide resistance in longitudinal samples obtained after continued enfuvirtide dosing post-virological failure. In 14th international drug resistance workshop, QC, Canada. Antiviral therapy, Suppl 1... [Pg.198]

Melby TE, Despirito M, Demasi RA, HeUek G, Thommes JA, Greenberg ML, Graham N (2007b) Association between specific enfuvirtide resistance mutations and CD4 cell response during enfuvirtide-based therapy. Aids 21 2537-2539... [Pg.199]

Covens K, Megens S, Dekeersmaeker N et al (2010) The rare HIV-1 gp41 mutations 43T and 50V elevate enfuvirtide resistance levels of common enfuvirtide resistance mutations that did not impact susceptibility to sifuvirtide. Antiviral Res 86 253-260... [Pg.160]

Dwyer JJ, Wilson KL, Davison DK et al (2007) Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus. Proc Natl Acad Sci USA 104 12772-12777... [Pg.160]

He Y, Cheng J, Lu H et al (2008) Potent HIV fusion inhibitors against enfuvirtide-resistant HIV-1 strains. Proc Natl Acad Sci USA 105 16332-16337... [Pg.160]

This chapter is intended to provide an overview of HIV-1 entry inhibitors, focusing on the mechanism of action, development, and knowledge of viral resistance to the currently available entry inhibitors, enfuvirtide and maraviroc. Although reversed relative to their order in the entry process, enfuvirtide is discussed first due to the greater clinical experience with this drug. [Pg.179]

Greenberg ML, Cammack N (2004) Resistance to enfuvirtide, the first HIV fusion inhibitor. J Antimicrob Chemother 54 333-340... [Pg.195]

Lalezari JP, Henry K, O Hearn M, Montaner JS, Piliero PJ, Trottier B, Walmsley S, Cohen C, Kuritzkes DR, Eron JJ Jr, Chung J, DeMasi R, Donatacci L, Drobnes C, Delehanty J, Salgo M (2003c) Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. N Engl J Med 348 2175-2185... [Pg.197]

Efficacy of enfuvirtide in patients infected with drag-resistant HIV-1 in Europe and Australia, N Engl J Med 348 2186-2195... [Pg.198]

Lu J, Sista P, Giguel F, Greenberg M, Kuritzkes DR (2004) Relative replicative fitness of human immunodeficiency virus type 1 mutants resistant to enfuvirtide (T-20), J Virol 78 4628 637 Lu M, Blacklow SC, Kim PS (1995) A tiimeric structural domain of the HlV-1 transmembrane glycoprotein, Nat Struct Biol 2 1075-1082... [Pg.198]

Poveda E, Rodes B, Lebel-Binay S, Faudon JL, Jimenez V, Soriano V (2005) Dynamics of enfuvir-tide resistance in HIV-infected patients during and after long-term enfuvirtide salvage therapy. J Clin Virol 34 295-301... [Pg.200]

Sista PR, Melby T, Davison D, Jin L, Mosier S, Mink M, Nelson EL, DeMasi R, Cammack N, Salgo MP, Matthews TJ, Greenberg ML (2004) Characterization of determinants of genotypic and phenotypic resistance to enfuvirtide in baseline and on-treatment HIV-1 isolates. Aids 18 1787-1794... [Pg.201]

Two classes of entry inhibitors have been developed. The first entry inhibitor approved as HIV therapy was enfuvirtide, a fusion inhibitor. In contrast with aU other antiretrovirals, this drug must be administered subcutaneously and twice a day, which represent important disadvantages to the patient. It is very potent and generally reserved for heavily antiretroviral-experienced patients with virologic failure. Unfortunately enfuvirtide shows a low genetic barrier for resistance (Fig. 2) and should be administered in combination with at least one other active drug. [Pg.336]

Resistance to enfuvirtide can occur as a result of mutations in gp41 codons the frequency and significance of this phenomenon are being investigated. However, enfuvirtide lacks cross-resistance to the other currently approved antiretroviral drug classes. [Pg.1082]

Resistance to maraviroc is associated with one or more mutations in the V3 loop of gpl20. There appears to be no cross-resistance with drugs from any other class, including the fusion inhibitor enfuvirtide. However, virologic failure of regimens containing maraviroc may potentially be caused not only by resistance but also by emergence... [Pg.1082]

Lalezari JP, Henry K, O Hearn M, Montaner JSG, et al. 2003. Enfuvirtide on HIV fusion inhibitor, for drug resistant HIV infection in North and South America. NEJM. 348 2175-2185. [Pg.199]

See other pages where Enfuvirtide Resistance is mentioned: [Pg.185]    [Pg.185]    [Pg.185]    [Pg.185]    [Pg.195]    [Pg.200]    [Pg.131]    [Pg.132]    [Pg.134]    [Pg.226]    [Pg.185]    [Pg.185]    [Pg.185]    [Pg.185]    [Pg.195]    [Pg.200]    [Pg.131]    [Pg.132]    [Pg.134]    [Pg.226]    [Pg.181]    [Pg.183]    [Pg.184]    [Pg.184]    [Pg.184]    [Pg.193]    [Pg.194]    [Pg.194]    [Pg.199]    [Pg.199]    [Pg.201]    [Pg.277]    [Pg.338]    [Pg.428]    [Pg.193]    [Pg.325]    [Pg.392]    [Pg.1990]    [Pg.609]    [Pg.609]   
See also in sourсe #XX -- [ Pg.185 ]

See also in sourсe #XX -- [ Pg.852 ]



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