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enfuvirtide

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Description

Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID16130199
CHEMBL ID525076
CHEBI ID608828
MeSH IDM0274523

Synonyms (46)

Synonym
gna & g-20
ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2 & hippeastrum hybrid agglutinin( hha)
humanized monoclonal antibody to cd4 & ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2
5a8 & t-20
hha & t-20
ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2 & galanthus nivalis agglutinin (gna)
tnx-355 & efuvirtide
enfuvirtide+pro 140
t-20+pro 140
ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2 & pro 140 (anti-ccr5 monoclonal antibody)
t20-lai
t-20-lai [ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2]
ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2
pentafuside
dp-178
T20 ,
acetyl-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2
r-698
t-20
fuzeon (tm)
dp178
gp41 127-162 aa
enfuvirtide
t 20
fuzeon
hsdb 7341
dp 178
t 20 (peptide)
enfuvirtide + t1144
t20 + t1144
CHEBI:608828 ,
actyrthrserleuilehisserleuileglugluserglnasnglnglnglulysasngluglngluleuleugluleuasplystrpalaserleutrpasntrpphenh2
pentafuside (trivial name)
CHEMBL525076
19owo1t3ze ,
unii-19owo1t3ze
enfuvirtide [usan:inn:ban]
bdbm50023615
fuzeon t-20
DTXSID20166672 ,
AKOS040763974
j05ax07
enfuvirtida
enfuvirtidum
enfuvirtide (mart.)
dtxcid8089163

Research Excerpts

Overview

Efuvirtide (T-20) is a peptide-based drug that targets the step of HIV fusion. As such, it effectively suppresses the replication of HIV-1 strains that are either wild type or resistant to reverse transcriptase and/or protease inhibitors. It requires very high (90 mg twice daily) therapeutic doses.

ExcerptReferenceRelevance
"Enfuvirtide (T-20) is a peptide-based drug that targets the step of HIV fusion, and as such, it effectively suppresses the replication of HIV-1 strains that are either wild type or resistant to multiple reverse transcriptase and/or protease inhibitors."( SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
Fujii, N; Izumi, K; Kajiwara, K; Kodama, E; Matsuoka, M; Naito, T; Nishikawa, H; Oishi, S; Sakagami, Y; Sarafianos, SG; Watanabe, K, 2009
)
1.27
"Enfuvirtide is a 36-residue synthetic peptide that targets gp41 and blocks viral fusion."( Evolved Proteins Inhibit Entry of Enfuvirtide-Resistant HIV-1.
Harris, RS; Ikeda, T; McNaughton, BR; Tennyson, RL; Walker, SN, 2019
)
1.51
"Enfuvirtide is a synthetic peptide that corresponds to 36 amino acids of the HR2, which competitively binds to HR1 inhibiting the interaction with the HR2 domain thus preventing fusogenic conformation and inhibiting viral entry into host cells."( Genetic analysis and natural polymorphisms in HIV-1 gp41 isolates from Maputo City, Mozambique.
Abreu, C; Bila, D; Ismael, N; Jani, I; Mabunda, N; Mariani, D; Tanuri, A; Vubil, A, 2014
)
1.12
"Enfuvirtide is a synthetic peptide that blocks the entry of HIV into healthy host CD4 cells, which requires very high (90 mg twice daily) therapeutic doses."( Gene fragment polymerization for increased yield of recombinant HIV fusion inhibitor enfuvirtide. [corrected].
Arva Tatireddigari, VR; Bajji, C; Gudipudi, A; Kosana, RR; Lomada, D; Narala, VR; Panati, K, 2014
)
1.35
"Enfuvirtide (ENF) is a clinically used peptide drug for the treatment of HIV infections, but its poor pharmacokinetic profile (T1/2 = 1.5 h in rats) and low aqueous solubility make the therapy expensive and inconvenience. "( Enfuvirtide-PEG conjugate: A potent HIV fusion inhibitor with improved pharmacokinetic properties.
Cheng, S; Gao, GF; Li, X; Lv, X; Ma, L; Shao, Y; Wang, Y; Zhang, Z, 2016
)
3.32
"Enfuvirtide is a potent inhibitor of systemic HIV-1 replication, but its penetration into the human central nervous system (CNS) has not been analysed. "( Enfuvirtide cerebrospinal fluid (CSF) pharmacokinetics and potential use in defining CSF HIV-1 origin.
Baker, B; Deeks, SG; Hoh, R; Kroll, JL; Kuritzkes, DR; Liegler, T; Parham, R; Price, RW; Sailstad, J; Spudich, S; Wring, SA, 2008
)
3.23
"Enfuvirtide (T-20) is a fusion inhibitor that suppresses replication of human immunodeficiency virus (HIV) variants with multi-drug resistance to reverse transcriptase and protease inhibitors. "( Design of peptide-based inhibitors for human immunodeficiency virus type 1 strains resistant to T-20.
Fujii, N; Ito, S; Izumi, K; Kitaura, K; Kodama, E; Matsuoka, M; Nishikawa, H; Oishi, S; Sakagami, Y; Sarafianos, SG; Shimura, K; Terakawa, Y; Watabe, T; Watanabe, K, 2009
)
1.8
"Enfuvirtide is a useful drug in those with reduced drug options."( A delayed hypersensitivity reaction to enfuvirtide after rechallenge.
Emerson, CR; Post, JJ; Workman, C, 2009
)
1.34
"Enfuvirtide is an attractive alternative to standard ARV therapy, facilitating the management of drug-drug interactions shortly after liver transplantation."( Enfuvirtide: a safe and effective antiretroviral agent for human immunodeficiency virus-infected patients shortly after liver transplantation.
Abbara, C; Antonini, T; Bonhomme-Faivre, L; Desbois, D; Duclos-Vallée, JC; Samuel, D; Teicher, E; Vittecoq, D, 2009
)
2.52
"Enfuvirtide (ENF) is a viral fusion inhibitor used in patients failing highly active antiretroviral therapy (HAART). "( High prevalence of primary Enfuvirtide (ENF) resistance-associated mutations in HIV-1-infected patients in Hong Kong.
Chan, KC; Chen, JH; Cheng, VC; Lam, HY; Leung, PH; Wong, KH; Yam, WC; Yuen, KY, 2010
)
2.1
"Enfuvirtide is a large protein that should be injected subcutaneously to ensure an appropriate absorption. "( Enfuvirtide administration in HIV-positive transgender patient with soft tissue augmentation: US evaluation.
Ferraioli, G; Ferraris, L; Filice, C; Gabrielli, E; Galli, M; Gervasoni, C; Riva, A, 2010
)
3.25
"Enfuvirtide (ENF) is an injectable entry/fusion inhibitor that is effective in achieving viral suppression when used in combination with protease inhibitors (PIs) in patients with pre-existing resistance."( A 48-week pilot study switching suppressed patients to darunavir/ritonavir and etravirine from enfuvirtide, protease inhibitor(s), and non-nucleoside reverse transcriptase inhibitor(s).
Alas, B; Perniciaro, A; Ruane, P; Ryan, R; Witek, J, 2010
)
1.3
"Enfuvirtide (T-20) is a novel antiretroviral agent that blocks HIV-1 cell fusion. "( The safety, plasma pharmacokinetics, and antiviral activity of subcutaneous enfuvirtide (T-20), a peptide inhibitor of gp41-mediated virus fusion, in HIV-infected adults.
Arduino, RC; Carlson, M; Cohen, C; Dusek, A; Eron, JJ; Gallant, JE; Goodgame, JC; Kilby, JM; Lalezari, JP; Murphy, RL; Nelson, EL; Saag, MS; Sista, PR; Valentine, F; Volberding, P, 2002
)
1.99
"Enfuvirtide is a synthetic peptide that binds to gp41, preventing the conformational change required for membrane fusion."( Enfuvirtide.
Chen, RY; Kilby, JM; Saag, MS, 2002
)
2.48
"Enfuvirtide is a novel antiretroviral that blocks HIV-1 cell fusion and viral entry. "( A controlled Phase II trial assessing three doses of enfuvirtide (T-20) in combination with abacavir, amprenavir, ritonavir and efavirenz in non-nucleoside reverse transcriptase inhibitor-naive HIV-infected adults.
Becker, S; Carlson, M; DeJesus, E; Delehanty, J; DeMasi, R; Haas, FF; Haubrich, R; Henry, D; Lalezari, JP; Northfelt, DW; Powderly, W; Richmond, G; Riddler, S; Salgo, M; Sista, PR; Thompson, M; Valentine, F; Wolfe, P; Wright, D, 2003
)
2.01
"Enfuvirtide is a fusion inhibitor used for the treatment of HIV-1 infection. "( Enfuvirtide: a novel agent for the treatment of HIV-1 infection.
Duffalo, ML; James, CW, 2003
)
3.2
"Enfuvirtide is an effective treatment option for HIV-1-infected individuals when used in combination with other antiretroviral agents. "( Enfuvirtide: a novel agent for the treatment of HIV-1 infection.
Duffalo, ML; James, CW, 2003
)
3.2
"Enfuvirtide is an addition to antiretroviral therapy since it targets a new step in the HIV life cycle."( Enfuvirtide, a new fusion inhibitor for therapy of human immunodeficiency virus infection.
Hardy, H; Skolnik, PR, 2004
)
2.49
"Enfuvirtide (Fuzeon) is an HIV fusion inhibitor, the first drug in a new class of antiretrovirals. "( Lack of interaction between enfuvirtide and ritonavir or ritonavir-boosted saquinavir in HIV-1-infected patients.
Bellibas, SE; Boyd, M; Buss, N; Dorr, A; Kinchelow, T; Kolis, S; Patel, IH; Ruxrungtham, K; Zhang, X, 2004
)
2.06
"Enfuvirtide is a peptide mimetic of an essential region within viral envelope glycoprotein gp41 that functions by blocking gp41 structural rearrangements at a transitional pre-fusion conformation."( Resistance to enfuvirtide, the first HIV fusion inhibitor.
Cammack, N; Greenberg, ML, 2004
)
1.41
"Enfuvirtide is a fusion inhibitor used for the treatment of HIV infection. "( Enfuvirtide (T-20): potentials and challenges.
Foy, K; Juethner, SN,
)
3.02
"Enfuvirtide is a 36 amino-acid synthetic peptide derived from the HR2 sequence of the HIV-1 gp41. "( [Enfuvirtide, first fusion inhibitor in the treatment of human immunodeficiency virus infection: mechanism of action and pharmacokinetics].
Raffi, F, 2004
)
2.68
"Enfuvirtide is a novel antiretroviral that is effective in HIV-infected patients whose treatment options are limited by multi-class antiretroviral resistance."( Enfuvirtide: a review of its use in the management of HIV infection.
Keating, GM; Oldfield, V; Plosker, G, 2005
)
2.49
"Enfuvirtide is a peptide derived from the HR2 region of the transmembrane glycoprotein from the HXB2 HIV-1 subtype B prototype strain that binds to the HR1 region."( Enfuvirtide binding domain is highly conserved in non-B HIV type 1 strains from Cameroon, West Central Africa.
Aghokeng, AF; Awazi, B; Delaporte, E; Ewane, L; Nanfack, A; Peeters, M; Zekeng, L, 2005
)
2.49
"Enfuvirtide is a new class of antiviral drug, fusion inhibitors, which interferate with penetration of HIV-1 in the cells. "( [Enfuvirtide, mechanism of action and pharmacological properties].
Becić, F; Kapić, E; Zvizdić, S, 2005
)
2.68
"Enfuvirtide is a good therapeutic option as rescue therapy in combination with other active antiretrovirals and works against different HIV-1 variants, including all group M subtypes and group O."( Enfuvirtide, the first fusion inhibitor to treat HIV infection.
Briz, V; Poveda, E; Soriano, V,
)
2.3
"Enfuvirtide (T20) is a peptide-based fusion inhibitor derived from the heptad repeat 2 (HR2) region of HIV-1 glycoprotein 41 (gp41). "( Heptad-repeat-2 mutations enhance the stability of the enfuvirtide-resistant HIV-1 gp41 hairpin structure.
Jenwitheesuk, E; Samudrala, R, 2005
)
2.02
"Enfuvirtide is an important component of antiretroviral therapy in highly treatment-experienced individuals where NRTI sparing may be desirable."( Enfuvirtide in HIV-1-infected individuals changing therapy to a nucleoside reverse transcriptase inhibitor sparing regimen: the ALLIANCE Study.
Amin, J; Cooper, D; Dwyer, DE; Hales, G; Miller, J; Workman, C, 2006
)
2.5
"Enfuvirtide is a virologically and immunologically active, injectable antiretroviral fusion inhibitor developed for the treatment of HIV infection. "( Enfuvirtide: patient acceptance and strategies for managing injection-site reactions.
Rice, C; Wilantewicz, H, 2006
)
3.22
"Enfuvirtide is a high-cost, parenterally administered drug commonly used in late phases of HIV infection, when its efficacy may be compromised. "( [Spanish recommendations for proper use of enfuvirtide].
Antela, A; Arazo, P; Arribas, JR; Cervantes, M; Domingo, P; Echevarría, S; Flores, J; Francés, A; Gómez-Sirvent, JL; González, J; Hernández-Quero, J; Lozano, F; Mallolas, J; Moreno, S; Muñoz, A; Ocampo, A; Portilla, J; Pulido, F; Ribera, E; Rivero, A; Santos, J; Soriano, V; Viciana, P, 2007
)
2.05
"Enfuvirtide is an effective treatment for HIV-1 infection in children and adolescents receiving optimized background therapy and has a favorable safety profile. "( Safety and efficacy of enfuvirtide for 48 weeks as part of an optimized antiretroviral regimen in pediatric human immunodeficiency virus 1-infected patients.
Bertasso, A; Church, J; Emmanuel, P; Eppes, S; Evans, C; Rowell, L; Wiznia, A, 2007
)
2.09

Effects

Efuvirtide has a new mode of action: it binds to the viral envelope glycoprotein 41 that is involved in the fusion of the virus to the membrane of the CD4 T cell. In clinical trials has been shown to exhibit high efficacy and low toxicity.

Efuvirtide has been shown to provide clinically relevant improvements in CD4 cell counts and reductions in HIV viraemia across all subgroups of treatment-experienced patients studied.

ExcerptReferenceRelevance
"Enfuvirtide has a new mode of action: it binds to the viral envelope glycoprotein 41 that is involved in the fusion of the virus to the membrane of the CD4 T cell."( [Enfuvirtide, the first representative of a new class of drugs for the treatment of HIV infection : HIV fusion inhibitors].
Koopmans, PP, 2003
)
1.95
"Enfuvirtide has a unique mechanism of action and high viral target specificity, and in clinical trials has been shown to exhibit both high efficacy and low toxicity."( Resistance to enfuvirtide, the first HIV fusion inhibitor.
Cammack, N; Greenberg, ML, 2004
)
1.41
"Enfuvirtide has been a cornerstone of salvage therapy for multidrug-resistant HIV. "( Outcomes of multidrug-resistant patients switched from enfuvirtide to raltegravir within a virologically suppressive regimen.
Harris, M; Larsen, G; Montaner, JS, 2008
)
2.04
"Enfuvirtide has been shown to provide clinically relevant improvements in CD4 cell counts and reductions in HIV viraemia across all subgroups of treatment-experienced patients studied, including those taking few or no other active drugs."( Clinical management of treatment-experienced, HIV-infected patients with the fusion inhibitor enfuvirtide: consensus recommendations.
Clotet, B; Cooper, D; Delfraissy, JF; Lazzarin, A; Moyle, G; Raffi, F; Rockstroh, J; Schapiro, J; Soriano, V, 2004
)
1.26
"Enfuvirtide (ENF) has been shown to improve short-term virologic responses when given to highly treatment-experienced patients with advanced HIV disease. "( Cost-effectiveness of enfuvirtide in treatment-experienced patients with advanced HIV disease.
Freedberg, KA; Goldie, SJ; Kimmel, AD; Losina, E; Muccio, TM; Paltiel, AD; Sax, PE; Walensky, RP; Weinstein, MC; Zhang, H, 2005
)
2.09

Treatment

In enfuvirtide-treated patients with virological suppression, there was no decay of the latent reservoir (95% confidence interval for half-life, 11 months to infinity). Enfuvirtside-based treatment regimens are associated with a rapid and durable response.

ExcerptReferenceRelevance
"In enfuvirtide-treated patients with virological suppression, there was no decay of the latent reservoir (95% confidence interval for half-life, 11 months to infinity)."( No evidence for decay of the latent reservoir in HIV-1-infected patients receiving intensive enfuvirtide-containing antiretroviral therapy.
Aga, E; Albrecht, M; Bastow, B; Bosch, RJ; Demeter, LM; Dykes, C; Eron, JJ; Gandhi, RT; Lai, J; Para, M; Siliciano, JD; Siliciano, RF, 2010
)
1.09
"Enfuvirtide-based treatment regimens are associated with a rapid and durable response. "( Week-12 response to therapy as a predictor of week 24, 48, and 96 outcome in patients receiving the HIV fusion inhibitor enfuvirtide in the T-20 versus Optimized Regimen Only (TORO) trials.
Chung, J; Katlama, C; Raffi, F; Saag, M; Salgo, M; Smiley, L; Wilkinson, M, 2006
)
1.98

Toxicity

Enfuvirtide was generally well tolerated, and no new patterns of adverse events compared with adults were observed. Injection site reactions were the most common adverse event, although they were rarely treatment-limiting.

ExcerptReferenceRelevance
"9%) of treatment-emergent adverse events were grade 2 or less in severity."( A phase II clinical study of the long-term safety and antiviral activity of enfuvirtide-based antiretroviral therapy.
Arduino, RC; Carlson, M; Cohen, C; DeJesus, E; Dusek, A; Eron, JJ; Gallant, JE; Kilby, JM; Lalezari, JP; Murphy, RL; Nelson, EL; Sista, PR; Valentine, F; Volberding, P, 2003
)
0.55
" Enfuvirtide was well tolerated, with injection site reactions being the most common adverse event, although they were rarely treatment-limiting."( Clinical safety and efficacy of enfuvirtide (T-20), a new fusion inhibitor. A review of the presentation at the satellite symposium "New hope: advancing care in HIV infection" at the 15th annual Association of Nurses in AIDS Care conference, November 2002
Lalezari, JP, 2003
)
1.51
" Parenteral administration of enfuvirtide in clinical trials has been safe and has resulted in significant decreases in plasma viral load, even in the setting of extensive previous treatment and multi-drug resistance to conventional antiretroviral (ARV) therapy."( Safety, tolerability, and plasma pharmacokinetics of high-strength formulations of enfuvirtide (T-20) in treatment-experienced HIV-1-infected patients.
Delehanty, J; DeMasi, R; Kilby, JM; Lalezari, JP; Patel, I; Salgo, M; Wheat, J; Wheeler, DA, 2004
)
0.84
" All cohorts had similar safety profiles and only one patient discontinued due to an adverse event."( Safety, tolerability, and plasma pharmacokinetics of high-strength formulations of enfuvirtide (T-20) in treatment-experienced HIV-1-infected patients.
Delehanty, J; DeMasi, R; Kilby, JM; Lalezari, JP; Patel, I; Salgo, M; Wheat, J; Wheeler, DA, 2004
)
0.55
" At each visit, each subject had a physical examination and an assessment for adverse events with particular attention to evaluation of injection site reactions."( Long term tolerability and safety of enfuvirtide for human immunodeficiency virus 1-infected children.
Chen, J; Church, JA; Cunningham, CK; Delora, P; Hawkins, E; Hughes, M; Mofenson, LM; Palumbo, P; Sista, P; Smith, E; Wiznia, A, 2004
)
0.6
" Two children experienced grade 3 adverse events resulting in discontinuation of the study drug; 1 subject developed grade 3 thrombocytopenia and 1 developed grade 3 edema at weeks 65 and 77, respectively."( Long term tolerability and safety of enfuvirtide for human immunodeficiency virus 1-infected children.
Chen, J; Church, JA; Cunningham, CK; Delora, P; Hawkins, E; Hughes, M; Mofenson, LM; Palumbo, P; Sista, P; Smith, E; Wiznia, A, 2004
)
0.6
"Enfuvirtide was generally safe and, except for a high rate of injection site reactions, well-tolerated in HIV-1-infected children for as long as 96 weeks."( Long term tolerability and safety of enfuvirtide for human immunodeficiency virus 1-infected children.
Chen, J; Church, JA; Cunningham, CK; Delora, P; Hawkins, E; Hughes, M; Mofenson, LM; Palumbo, P; Sista, P; Smith, E; Wiznia, A, 2004
)
2.04
"6% to the control group discontinued study treatment before week 48; the percentage of patients withdrawn for safety reasons (including adverse events [AEs], deaths, and laboratory abnormalities) was 14."( Safety of enfuvirtide in combination with an optimized background of antiretrovirals in treatment-experienced HIV-1-infected adults over 48 weeks.
Arastéh, K; Atkins, B; Bader-Weder, S; Bertasso, A; Bourdeau, L; Chung, J; Clotet, B; Cohen, C; Cooper, D; Delfraissy, JF; Demasi, R; Drobnes, C; Eron, JJ; Guimaraes, D; Henry, K; Hughes, F; Katlama, C; Kinchelow, T; Kuritzkes, D; Labriola-Tompkins, E; Lalezari, J; Lange, J; Lazzarin, A; Montaner, J; Natale, C; Nelson, M; O'Hearn, M; Piliero, P; Reynes, J; Salgo, MP; Shikhman, A; Smiley, L; Stellbrink, HJ; Trottier, B; Walmsley, S, 2005
)
0.73
" There were no significant differences in adverse events between the two dosing regimens."( Pharmacokinetics, pharmacodynamics and safety of once-daily versus twice-daily dosing with enfuvirtide in HIV-infected subjects.
Chiu, YY; DeJesus, E; Flaherty, J; McFalls, E; Miralles, GD; Patel, IH; Piliero, P; Richmond, G; Thompson, M; True, A; Wheeler, D; Zhang, Y, 2006
)
0.55
" The type and frequency of adverse events were much the same in the two groups."( 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.
Baeten, B; Beets, G; Campbell, T; Clotet, B; de Smedt, G; Johnson, M; Katlama, C; Lazzarin, A; Moll, A; Peeters, M; Sinha, R; Towner, W; Trottier, B; Vingerhoets, J; Woodfall, B, 2007
)
0.34
"Enfuvirtide was generally well tolerated, and no new patterns of adverse events compared with adults were observed."( Safety and efficacy of enfuvirtide for 48 weeks as part of an optimized antiretroviral regimen in pediatric human immunodeficiency virus 1-infected patients.
Bertasso, A; Church, J; Emmanuel, P; Eppes, S; Evans, C; Rowell, L; Wiznia, A, 2007
)
2.09
" The proportion reporting 1 adverse event or ISRs was comparable between arms, despite an increased incidence of grade 4 erythema (13% vs."( Efficacy and safety of 48 weeks of enfuvirtide 180 mg once-daily dosing versus 90 mg twice-daily dosing in HIV-infected patients.
Chiu, YY; Chung, J; Demasi, R; Donatacci, L; Godofsky, E; Graham, N; Labriola-Tompkins, E; Rodriguez, A; Rowell, L; Salgo, M; Shikhman, A; Tucker, E; Walmsley, S; Wright, D,
)
0.41
" Haematoma was the sole NFID-related serious adverse event, but this did not lead to discontinuation."( Short communication safety, tolerability and pharmacokinetics of enfuvirtide administered by a needle-free injection system compared with subcutaneous injection.
Gottlieb, M; Thommes, JA, 2008
)
0.58
"Compared with a standard NS, use of an NFID to administer ENF was associated with a substantially lower incidence of painful ISRs, was generally safe and well-tolerated, and was preferred by most participants in the study."( Short communication safety, tolerability and pharmacokinetics of enfuvirtide administered by a needle-free injection system compared with subcutaneous injection.
Gottlieb, M; Thommes, JA, 2008
)
0.58
" Ibalizumab was not immunogenic, and no serious drug-related adverse effects occurred."( Safety, pharmacokinetics, and antiretroviral activity of multiple doses of ibalizumab (formerly TNX-355), an anti-CD4 monoclonal antibody, in human immunodeficiency virus type 1-infected adults.
DeJesus, E; Godofsky, E; Jacobson, JM; Kuritzkes, DR; Larson, JA; Lewis, ST; Weinheimer, SP, 2009
)
0.35
" There is a complex, combined effect of HIV infection plus antiretroviral treatment on the incidence of gastrointestinal symptoms, and, for some trials, the majority of gastrointestinal adverse events may not be related to antiretroviral treatment."( Risk factors for gastrointestinal adverse events in HIV treated and untreated patients.
Balkin, A; Hill, A,
)
0.13
" Adverse events did not need to stop or change HAART."( Efficacy and safety of a salvage regimen based on tipranavir, enfuvirtide and three nucleoside analogues in HIV1 infected patients with clinical progression: 96-week evaluation.
Consorte, A; Cosentino, L; D'Annunzio, M; Di Giammartino, D; Di Masi, F; Falconi, L; Parruti, G; Polilli, E; Sozio, F; Tontodonati, M, 2009
)
0.59
" There were no grade 3 or 4 adverse events related to raltegravir."( Efficacy and safety of switching from enfuvirtide to raltegravir in patients with virological suppression.
Caum, C; Clotet, B; Domingo, P; Ferrer, E; Imaz, A; Llibre, JM; Martin-Iguacel, R; Moltó, J; Podzamczer, D; Santos, JR,
)
0.4
" Six patients prematurely withdrew from the present study in which three expired from HIV related complications, two withdrew consents, and one from adverse event."( Two-year safety and tolerability study of enfuvertide use in salvage therapy of Thai HIV-1 experienced cases.
Anekthananon, T; Hanvanich, M; Prasithsirikul, W; Ratanasuwan, W; Supparatpinyo, K; Suwanagool, S; Techasathit, W; Viphagool, A, 2011
)
0.37
" The adverse events did not compromise the patient compliance."( Two-year safety and tolerability study of enfuvertide use in salvage therapy of Thai HIV-1 experienced cases.
Anekthananon, T; Hanvanich, M; Prasithsirikul, W; Ratanasuwan, W; Supparatpinyo, K; Suwanagool, S; Techasathit, W; Viphagool, A, 2011
)
0.37
"In absence of HIV infection, or concomitant treatment, short-term exposure to T20 or RAL in healthy adult volunteers did not lead to any indicative changes in toxicity markers thus presuming the safe profile of both drugs."( Metabolic, mitochondrial, renal and hepatic safety of enfuvirtide and raltegravir antiretroviral administration: Randomized crossover clinical trial in healthy volunteers.
Arnaiz, JA; Barroso, S; Blanco, JL; Carné, X; Garrabou, G; Gatell, JM; González-Segura, À; Larousse, M; Lazzari, E; Llopis, J; Loncà, M; Mallolas, J; Manriquez, M; Martínez, E; Miró, O; Morén, C; Riba, N; Santana, G, 2019
)
0.76

Pharmacokinetics

Enfuvirtide was nearly completely absorbed from subcutaneous depot, and pharmacokinetic parameters were linear up to a dose of 180 mg in this study. There was no significant difference between children and adolescents for enfvirtide Cmax (6.5)

ExcerptReferenceRelevance
" The objectives of this study were to develop a structural pharmacokinetic model that would adequately characterize the absorption and disposition of enfuvirtide pharmacokinetics after both intravenous and subcutaneous administration and to evaluate the dose proportionality of enfuvirtide pharmacokinetic parameters at a subcutaneous dose higher than that currently used in phase III studies."( Pharmacokinetics of plasma enfuvirtide after subcutaneous administration to patients with human immunodeficiency virus: Inverse Gaussian density absorption and 2-compartment disposition.
Dorr, A; Kinchelow, T; Kolis, S; Lang, JM; Nieforth, K; Patel, IH; Reynes, J; Rouzier-Panis, R; Stiles, MR; Zhang, X, 2002
)
0.81
" The model-derived mean pharmacokinetic parameters (+/-SD) were volume of distribution of the central compartment (3."( Pharmacokinetics of plasma enfuvirtide after subcutaneous administration to patients with human immunodeficiency virus: Inverse Gaussian density absorption and 2-compartment disposition.
Dorr, A; Kinchelow, T; Kolis, S; Lang, JM; Nieforth, K; Patel, IH; Reynes, J; Rouzier-Panis, R; Stiles, MR; Zhang, X, 2002
)
0.61
" Enfuvirtide was nearly completely absorbed from subcutaneous depot, and pharmacokinetic parameters were linear up to a dose of 180 mg in this study."( Pharmacokinetics of plasma enfuvirtide after subcutaneous administration to patients with human immunodeficiency virus: Inverse Gaussian density absorption and 2-compartment disposition.
Dorr, A; Kinchelow, T; Kolis, S; Lang, JM; Nieforth, K; Patel, IH; Reynes, J; Rouzier-Panis, R; Stiles, MR; Zhang, X, 2002
)
1.52
" The ratios of least squares means (LSM) and 90% confidence intervals for enfuvirtide and enfuvirtide metabolite pharmacokinetic parameters (AUC12h, Cmax, Ctrough) were estimated in the presence and absence of rifampicin."( Lack of enzyme-inducing effect of rifampicin on the pharmacokinetics of enfuvirtide.
Boyd, MA; Buss, N; Dorr, A; Kinchelow, T; Kolis, S; Nieforth, K; Patel, IH; Ruxrungtham, K; Zhang, X, 2003
)
0.78
"A 1-compartment population pharmacokinetic model with first-order absorption and elimination was fit to subcutaneous and intravenous dose pharmacokinetic data from a 2-part study, as follows: an intensive-sample pharmacokinetic design (observed dose) (subcutaneous and intravenous, n = 12) followed by a sparse-sample design (unobserved dose) (subcutaneous, n = 15)."( Population pharmacokinetics of enfuvirtide in pediatric patients with human immunodeficiency virus: searching for exposure-response relationships.
Aweeka, FT; Church, JA; Cunningham, CK; Kosel, BW; Palumbo, P; Sheiner, LB; Soy, D, 2003
)
0.6
" Time after the beginning of therapy did not significantly affect any pharmacokinetic parameter, supporting the absence of metabolic induction and inhibition."( Population pharmacokinetics of enfuvirtide in pediatric patients with human immunodeficiency virus: searching for exposure-response relationships.
Aweeka, FT; Church, JA; Cunningham, CK; Kosel, BW; Palumbo, P; Sheiner, LB; Soy, D, 2003
)
0.6
" Pharmacokinetic data indicated that the high-strength 100 mg/ml CO(3) formulation was bioequivalent to the 50 mg/ml CO(3) formulation whereas the TRIS formulation was not."( Safety, tolerability, and plasma pharmacokinetics of high-strength formulations of enfuvirtide (T-20) in treatment-experienced HIV-1-infected patients.
Delehanty, J; DeMasi, R; Kilby, JM; Lalezari, JP; Patel, I; Salgo, M; Wheat, J; Wheeler, DA, 2004
)
0.55
" Because the patient's pharmacokinetic profile was not significantly altered, compared with that of HIV-infected patients with normal renal function, no dose modifications were required."( Pharmacokinetics of enfuvirtide in a patient with impaired renal function.
Leen, C; Nieforth, K; Wat, C, 2004
)
0.65
"There was no significant difference between children and adolescents for enfuvirtide Cmax (6."( Pharmacokinetics of enfuvirtide in pediatric human immunodeficiency virus 1-infected patients receiving combination therapy.
Bellibas, SE; Bertasso, A; Cotler, S; Delora, P; Dorr, A; Kolis, SJ; Siddique, Z; Sista, P, 2004
)
0.88
"3%) and the elimination half-life (3."( Pharmacokinetics, pharmacodynamics and drug interaction potential of enfuvirtide.
Buss, N; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.56
"5 microg/ml Cmax between 5 and 7 hours."( [Enfuvirtide, first fusion inhibitor in the treatment of human immunodeficiency virus infection: mechanism of action and pharmacokinetics].
Raffi, F, 2004
)
1.23
" NONMEM software was used for population pharmacokinetic analysis and to assess the effects of age, gender, body weight, anti-gp41 antibodies, and concomitant drugs."( Population pharmacokinetics and exposure-response relationship of enfuvirtide in treatment-experienced human immunodeficiency virus type 1-infected patients.
Buss, N; Mould, DR; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.57
"An on-line SPE-LC/MS/MS approach was established for peptide pharmacokinetic studies."( Pharmacokinetics of sifuvirtide, a novel anti-HIV-1 peptide, in monkeys and its inhibitory concentration in vitro.
Dai, SJ; Dou, GF; Liang, Q; Liu, DS; Liu, XW; Qiang, XH; Song, HF; Tang, ZM; Yang, LM; Zheng, YT, 2005
)
0.33
" The median maximum concentration of drug in serum (Cmax) of 3,943 ng/ml, predicted for 3 h after drug administration, is lower than the Cmax reported previously."( Pharmacokinetics of enfuvirtide in patients treated in typical routine clinical settings.
Arastéh, K; Breske, A; Goebel, F; Herzmann, C; Kloft, C; Kreckel, P; Kruse, G; Kurowski, M; Moecklinghoff, C; Plettenberg, A; Plock, N; Roeling, J; Schulbin, H; Staszewski, S; Stocker, H; Weber, C, 2006
)
0.66
"Steady-state intensive pharmacokinetic samples were obtained on days 7 and 14."( Pharmacokinetics, pharmacodynamics and safety of once-daily versus twice-daily dosing with enfuvirtide in HIV-infected subjects.
Chiu, YY; DeJesus, E; Flaherty, J; McFalls, E; Miralles, GD; Patel, IH; Piliero, P; Richmond, G; Thompson, M; True, A; Wheeler, D; Zhang, Y, 2006
)
0.55
" Linear regression analysis suggested that decline in viral load up to day 7 was associated with Ctrough but not Cmax or AUC."( Pharmacokinetics, pharmacodynamics and safety of once-daily versus twice-daily dosing with enfuvirtide in HIV-infected subjects.
Chiu, YY; DeJesus, E; Flaherty, J; McFalls, E; Miralles, GD; Patel, IH; Piliero, P; Richmond, G; Thompson, M; True, A; Wheeler, D; Zhang, Y, 2006
)
0.55
" NONMEM was used for population pharmacokinetic analysis."( Population pharmacokinetics of enfuvirtide in HIV-1-infected pediatric patients over 48 weeks of treatment.
Bertasso, A; Dorr, A; Evans, C; Kolis, SJ; Lin, T; Patel, I; Salgo, M; Zhang, X, 2007
)
0.63
" After each dose, a full 48-hour pharmacokinetic profile was collected and pharmacokinetic parameters were estimated using model-independent techniques."( Enfuvirtide does not require dose adjustment in patients with chronic kidney failure: results of a pharmacokinetic study of enfuvirtide in HIV-1-infected patients with impaired kidney function.
Bellos, N; Chiu, YY; Evans, C; Godofsky, E; Lucasti, C; Patel, I; Richmond, G; Rowell, L; Salgo, M; Tebas, P, 2008
)
1.79
"3 microg h/mL) and Cmax (5."( Enfuvirtide does not require dose adjustment in patients with chronic kidney failure: results of a pharmacokinetic study of enfuvirtide in HIV-1-infected patients with impaired kidney function.
Bellos, N; Chiu, YY; Evans, C; Godofsky, E; Lucasti, C; Patel, I; Richmond, G; Rowell, L; Salgo, M; Tebas, P, 2008
)
1.79
"Enfuvirtide exposure observed in patients with ESRD requiring dialysis or chronic kidney disease was slightly higher than in patients with normal kidney function and similar to historical Cmax and AUC values from studies in patients with normal kidney function."( Enfuvirtide does not require dose adjustment in patients with chronic kidney failure: results of a pharmacokinetic study of enfuvirtide in HIV-1-infected patients with impaired kidney function.
Bellos, N; Chiu, YY; Evans, C; Godofsky, E; Lucasti, C; Patel, I; Richmond, G; Rowell, L; Salgo, M; Tebas, P, 2008
)
3.23
" Further, our model reveals that key pharmacokinetic characteristics of enfuvirtide, viz."( Mechanism-based model of the pharmacokinetics of enfuvirtide, an HIV fusion inhibitor.
Dixit, NM; Mohanty, U, 2008
)
0.83
" We performed a pharmacokinetic profile in a pregnant woman with multidrug-resistant HIV-1 infection at 37 weeks gestation."( Pharmacokinetic profile in late pregnancy and cord blood concentration of tipranavir and enfuvirtide.
Feiterna-Sperling, C; Hoffmeister, B; Kurowski, M; Schürmann, D; Weizsaecker, K, 2011
)
0.59
" More comprehensive in vivo pharmacokinetic data are required to justify the potential use of these agents as safe and effective options during pregnancy."( Pharmacokinetics of antiretroviral drugs in anatomical sanctuary sites: the fetal compartment (placenta and amniotic fluid).
Back, DJ; Else, LJ; Khoo, SH; Taylor, S, 2011
)
0.37
"5 h for 20 mg group; the mean Cmax of last dose was 498 ± 54 ng/mL for 10 mg group and 897 ± 136 ng/mL for 20 mg group."( Pharmacokinetics of sifuvirtide in treatment-naive and treatment-experienced HIV-infected patients.
Che, J; Chen, X; Cheng, Y; Dong, T; Meng, Q; Qian, X; Tong, B, 2014
)
0.4
"Enfuvirtide (ENF) is a clinically used peptide drug for the treatment of HIV infections, but its poor pharmacokinetic profile (T1/2 = 1."( Enfuvirtide-PEG conjugate: A potent HIV fusion inhibitor with improved pharmacokinetic properties.
Cheng, S; Gao, GF; Li, X; Lv, X; Ma, L; Shao, Y; Wang, Y; Zhang, Z, 2016
)
3.32

Compound-Compound Interactions

ExcerptReferenceRelevance
" The pharmacokinetic-pharmacodynamic relationship indicates that the recommended dose, in combination with other active antiretrovirals, is optimal."( Pharmacokinetics, pharmacodynamics and drug interaction potential of enfuvirtide.
Buss, N; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.56
" This unexpected drug-drug interaction warrants further investigation."( Unexpected drug-drug interaction between tipranavir/ritonavir and enfuvirtide.
Bargiacchi, O; Bonora, S; Calcagno, A; D'Avolio, A; Di Perri, G; González de Requena, D; Ladetto, L; Sciandra, M; Siccardi, M; Sinicco, A, 2006
)
0.57
" Clinically significant drug interactions were defined as drug interactions that required a dosage adjustment or consisted of a drug combination that is contraindicated due to its high potential for clinical adverse effects."( Prevalence and risk factors for clinically significant drug interactions with antiretroviral therapy.
El-Kholi, R; Faragon, JJ; Lodise, TP; Miller, CD, 2007
)
0.34
" This prospective, open-label, 24-week, single-arm trial assessed the efficacy and safety of enfuvirtide (90 mg injected subcutaneously twice daily) in combination with darunavir-ritonavir (600/100 mg administered orally twice daily) in triple-antiretroviral-class-experienced adults failing their current regimen."( Safety and efficacy of enfuvirtide in combination with darunavir-ritonavir and an optimized background regimen in treatment-experienced human immunodeficiency virus-infected patients: the below the level of quantification study.
DeJesus, E; Gathe, JC; Gottlieb, MS; Greenberg, ML; Guittari, CJ; Zolopa, AR, 2008
)
0.88

Bioavailability

The relative bioavailability of enfuvirtide, based on AUC12h and abdomen as a reference site, was 101% for thigh and 117% for arm.

ExcerptReferenceRelevance
"1 L/h), bioavailability (89% +/- 11%), and mean absorption time (7."( Pharmacokinetics of plasma enfuvirtide after subcutaneous administration to patients with human immunodeficiency virus: Inverse Gaussian density absorption and 2-compartment disposition.
Dorr, A; Kinchelow, T; Kolis, S; Lang, JM; Nieforth, K; Patel, IH; Reynes, J; Rouzier-Panis, R; Stiles, MR; Zhang, X, 2002
)
0.61
"The primary objective of this study was to determine the steady-state pharmacokinetics and relative bioavailability of enfuvirtide following sc injection at three separate anatomical sites: abdomen (A), thigh (B) and arm (C)."( Influence of subcutaneous injection site on the steady-state pharmacokinetics of enfuvirtide (T-20) in HIV-1-infected patients.
Dorr, A; Hawker, N; Kinchelow, T; Kolis, SJ; Lalezari, JP; Patel, IH; Siddique, Z; Zhang, X, 2003
)
0.75
"The relative bioavailability of enfuvirtide, based on AUC12h and abdomen as a reference site, was 101% for thigh and 117% for arm."( Influence of subcutaneous injection site on the steady-state pharmacokinetics of enfuvirtide (T-20) in HIV-1-infected patients.
Dorr, A; Hawker, N; Kinchelow, T; Kolis, SJ; Lalezari, JP; Patel, IH; Siddique, Z; Zhang, X, 2003
)
0.83
" The parameters of this model are clearance (CL), volume of distribution (V), absorption rate (k(a)), bioavailability (F), and both interindividual and residual variability."( Population pharmacokinetics of enfuvirtide in pediatric patients with human immunodeficiency virus: searching for exposure-response relationships.
Aweeka, FT; Church, JA; Cunningham, CK; Kosel, BW; Palumbo, P; Sheiner, LB; Soy, D, 2003
)
0.6
" Absolute bioavailability after subcutaneous injection is 84%."( Enfuvirtide: first fusion inhibitor for treatment of HIV infection.
Jamjian, MC; McNicholl, IR, 2004
)
1.77
" Bioavailability is high (84."( Pharmacokinetics, pharmacodynamics and drug interaction potential of enfuvirtide.
Buss, N; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.56
"4 microg/ml and the bioavailability of the drug is approximately 80%."( [Enfuvirtide, first fusion inhibitor in the treatment of human immunodeficiency virus infection: mechanism of action and pharmacokinetics].
Raffi, F, 2004
)
1.23
"25-2 h, and the absolute bioavailability was 49%+/-13%."( Pharmacokinetics of sifuvirtide, a novel anti-HIV-1 peptide, in monkeys and its inhibitory concentration in vitro.
Dai, SJ; Dou, GF; Liang, Q; Liu, DS; Liu, XW; Qiang, XH; Song, HF; Tang, ZM; Yang, LM; Zheng, YT, 2005
)
0.33
"To compare the relative bioavailability of enfuvirtide, a human immunodeficiency virus type 1 (HIV-1) fusion inhibitor, injected with the Biojector 2000 (B2000) needle-free device versus a 27-gauge half-inch needle-syringe; and to assess safety, tolerability, and patient preference for the two devices."( Pharmacokinetic bioequivalence of enfuvirtide using a needle-free device versus standard needle administration.
Chiu, YY; Demasi, RA; Patel, I; Stout, R; True, AL, 2006
)
0.88

Dosage Studied

Larger and longer-term studies are needed to determine if 180 mg once daily is an effective dosing alternative. The pharmacokinetic profile of subcutaneously administered enfuvirtide allows for twice-daily administration, although the possibility of once-daily dosing has not been excluded.

ExcerptRelevanceReference
" Plasma virus derived from patients enrolled in all dosage groups of the phase I T-20 trial was analyzed by population sequencing before and after treatment."( Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy.
Arani, RB; Decker, JM; Kappes, JC; Kilby, JM; Liu, H; Saag, MS; Shaw, GM; Wei, X; Wu, X; Zhang, Z, 2002
)
0.31
" Phase 2 studies established subcutaneous injection of 100 mg of enfuvirtide twice daily as the dosage of choice."( Clinical safety and efficacy of enfuvirtide (T-20), a new fusion inhibitor. A review of the presentation at the satellite symposium "New hope: advancing care in HIV infection" at the 15th annual Association of Nurses in AIDS Care conference, November 2002
Lalezari, JP, 2003
)
0.84
"These findings indicate that most patients taking enfuvirtide in clinical trials learn to integrate enfuvirtide dosing in their daily routines; with appropriate education and training, enfuvirtide self-injection becomes routine with relatively little subjective impact on daily functioning and activities of daily living."( Patient acceptance of self-injected enfuvirtide at 8 and 24 weeks.
Cohen, C; Green, J; Hellinger, J; Johnson, M; Patel, K; Staszewski, S; Wintfeld, N,
)
0.66
" The approved dosage is 90 mg twice/day by subcutaneous injection in adults and 2 mg/kg twice/day in children older than 6 years."( Enfuvirtide, a new fusion inhibitor for therapy of human immunodeficiency virus infection.
Hardy, H; Skolnik, PR, 2004
)
1.77
" The recommended dosage of enfuvirtide is 90 mg SC BID in adults and 2 mg/kg SC BID in children."( Enfuvirtide: a fusion inhibitor for the treatment of HIV infection.
Fung, HB; Guo, Y, 2004
)
2.06
" The pharmacokinetic profile of subcutaneously administered enfuvirtide allows for twice-daily administration, although the possibility of once-daily dosing has not been excluded."( Enfuvirtide.
Lalezari, JP; Luber, AD, 2004
)
2.01
" Thus, no dosage adjustments are warranted when enfuvirtide is coadministered with low-dose ritonavir or saquinavir boosted with a low dose of ritonavir."( Lack of interaction between enfuvirtide and ritonavir or ritonavir-boosted saquinavir in HIV-1-infected patients.
Bellibas, SE; Boyd, M; Buss, N; Dorr, A; Kinchelow, T; Kolis, S; Patel, IH; Ruxrungtham, K; Zhang, X, 2004
)
0.87
" A post hoc regression analysis based on AUC12 hours showed that body weight-adjusted dosing of enfuvirtide provides drug exposure that is independent of age group, body weight and body surface area."( Pharmacokinetics of enfuvirtide in pediatric human immunodeficiency virus 1-infected patients receiving combination therapy.
Bellibas, SE; Bertasso, A; Cotler, S; Delora, P; Dorr, A; Kolis, SJ; Siddique, Z; Sista, P, 2004
)
0.87
" Enfuvirtide clearance is influenced to a small extent by sex and bodyweight but this does not necessitate dosage adjustment."( Pharmacokinetics, pharmacodynamics and drug interaction potential of enfuvirtide.
Buss, N; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
1.47
" Antiviral response to enfuvirtide was independent of drug exposure, suggesting that the approved 90-mg twice-daily dose was in the plateau portion of the dose-response curve."( Population pharmacokinetics and exposure-response relationship of enfuvirtide in treatment-experienced human immunodeficiency virus type 1-infected patients.
Buss, N; Mould, DR; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.88
" Efficacy reached a plateau at the 90-mg twice-daily dosage in the exposure-response curve."( Population pharmacokinetics and exposure-response relationship of enfuvirtide in treatment-experienced human immunodeficiency virus type 1-infected patients.
Buss, N; Mould, DR; Nieforth, K; Patel, IH; Salgo, M; Zhang, X, 2005
)
0.57
" The PK model was used for simulations resulting in percentile curves for ENF levels for the full dosing interval."( Pharmacokinetics of enfuvirtide in patients treated in typical routine clinical settings.
Arastéh, K; Breske, A; Goebel, F; Herzmann, C; Kloft, C; Kreckel, P; Kruse, G; Kurowski, M; Moecklinghoff, C; Plettenberg, A; Plock, N; Roeling, J; Schulbin, H; Staszewski, S; Stocker, H; Weber, C, 2006
)
0.66
" Thirty-three subjects completed both dosing periods."( Pharmacokinetics, pharmacodynamics and safety of once-daily versus twice-daily dosing with enfuvirtide in HIV-infected subjects.
Chiu, YY; DeJesus, E; Flaherty, J; McFalls, E; Miralles, GD; Patel, IH; Piliero, P; Richmond, G; Thompson, M; True, A; Wheeler, D; Zhang, Y, 2006
)
0.55
" Larger and longer-term studies are needed to determine if 180 mg once daily is an effective dosing alternative for enfuvirtide."( Pharmacokinetics, pharmacodynamics and safety of once-daily versus twice-daily dosing with enfuvirtide in HIV-infected subjects.
Chiu, YY; DeJesus, E; Flaherty, J; McFalls, E; Miralles, GD; Patel, IH; Piliero, P; Richmond, G; Thompson, M; True, A; Wheeler, D; Zhang, Y, 2006
)
0.76
" The medications, including their pharmacokinetic properties, side effects, and dosing are reviewed."( Antiretroviral therapy 2006: pharmacology, applications, and special situations.
Bettiker, R; Samuel, R; Suh, B, 2006
)
0.33
" However, early HAART often consisted of drugs with complex dosing schedules, strict food requirements, treatment-limiting adverse effects, and the need to take 16-20 pills/day."( An update and review of antiretroviral therapy.
Piacenti, FJ, 2006
)
0.33
" It is approved for use in adults and dosage recommendations exist for children aged 6 years or older."( Safety and efficacy of enfuvirtide for 48 weeks as part of an optimized antiretroviral regimen in pediatric human immunodeficiency virus 1-infected patients.
Bertasso, A; Church, J; Emmanuel, P; Eppes, S; Evans, C; Rowell, L; Wiznia, A, 2007
)
0.65
" Clinically significant drug interactions were defined as drug interactions that required a dosage adjustment or consisted of a drug combination that is contraindicated due to its high potential for clinical adverse effects."( Prevalence and risk factors for clinically significant drug interactions with antiretroviral therapy.
El-Kholi, R; Faragon, JJ; Lodise, TP; Miller, CD, 2007
)
0.34
" Thus, enfuvirtide does not require dosage adjustment in patients with impaired kidney function."( Enfuvirtide does not require dose adjustment in patients with chronic kidney failure: results of a pharmacokinetic study of enfuvirtide in HIV-1-infected patients with impaired kidney function.
Bellos, N; Chiu, YY; Evans, C; Godofsky, E; Lucasti, C; Patel, I; Richmond, G; Rowell, L; Salgo, M; Tebas, P, 2008
)
2.24
" Here we present prospectively planned longitudinal analyses of FI resistance during 48 weeks of T-1249 dosing in patients with extensive prior FI exposure."( Evolution of genotypic and phenotypic resistance during chronic treatment with the fusion inhibitor T-1249.
Cammack, N; Demasi, R; Greenberg, ML; Melby, T; Miralles, GD, 2007
)
0.34
", steady state values of peak and trough concentrations and area under the concentration-time curve, vary nearly linearly with dosage over a broad range of dosages and for different dosing regimens, which enables a priori estimation of enfuvirtide exposure levels for different treatment protocols and may serve to establish guidelines for therapy optimization."( Mechanism-based model of the pharmacokinetics of enfuvirtide, an HIV fusion inhibitor.
Dixit, NM; Mohanty, U, 2008
)
0.78
" This bioconjugate, PC-1505, was designed to require less frequent dosing and less peptide than T-20 and was assessed for its antifusogenic activity both in vitro and in vivo in the SCID-hu Thy/Liv mouse model."( Albumin-conjugated C34 peptide HIV-1 fusion inhibitor: equipotent to C34 and T-20 in vitro with sustained activity in SCID-hu Thy/Liv mice.
Bakis, P; Bellomo, M; Bousquet-Gagnon, N; Bridon, D; Galkina, SA; Liscourt, P; Lobach, A; Mankowski, MK; Nault, G; Paradis, V; Ptak, RG; Quraishi, O; Rivard, ME; Robitaille, M; Stoddart, CA; Thibaudeau, K, 2008
)
0.35
" These findings suggest that application of enfuvirtide and sifuvirtide in combination may improve their efficacy and resistant profile, leading to a reduction of the dosage and frequency of drug use."( Synergistic efficacy of combination of enfuvirtide and sifuvirtide, the first- and next-generation HIV-fusion inhibitors.
Jiang, S; Lu, H; Pan, C; Qi, Z, 2009
)
0.88
" Providers should be aware of the need for tropism determination and dosing requirements for maraviroc."( Novel drug classes: entry inhibitors [enfuvirtide, chemokine (C-C motif) receptor 5 antagonists].
McKinnell, JA; Saag, MS, 2009
)
0.62
" We determine analytical thresholds for the dosage and dosing intervals to ensure the disease-free equilibrium remains stable."( Modelling the effects of adherence to the HIV fusion inhibitor enfuvirtide.
Lou, J; Smith, RJ, 2011
)
0.61
" However, ENF treatment is associated with injection site reactions and dosing fatigue."( A 48-week pilot study switching suppressed patients to darunavir/ritonavir and etravirine from enfuvirtide, protease inhibitor(s), and non-nucleoside reverse transcriptase inhibitor(s).
Alas, B; Perniciaro, A; Ruane, P; Ryan, R; Witek, J, 2010
)
0.58
" The 50% inhibitory concentration (IC(50)), 90% inhibitory concentration (IC(90)) and dose-response curve slopes were determined for each drug."( Baseline susceptibility of primary HIV-2 to entry inhibitors.
Antunes, F; Barroso, H; Bártolo, I; Borrego, P; Caixas, U; Calado, R; Cavaco-Silva, P; Doroana, M; Maltez, F; Marcelino, JM; Rocha, C; Taveira, N, 2012
)
0.38
"Enfuvirtide was selected as a test compound and dosed intravenously at 2 mg/kg to rats."( Identifying metabolite ions of peptide drugs in the presence of an in vivo matrix background.
Bockx, M; Cools, W; Cuyckens, F; de Vries, R; Dillen, L; Mortishire-Smith, RJ; Vereyken, L, 2012
)
1.82
" Food and Drug Administration, enfuvirtide is rarely used in combination antiretroviral therapies (cART) to treat HIV-1 infection, primarily because of its intense dosing schedule that requires twice-daily subcutaneous injection."( In vitro characterization of a sustained-release formulation for enfuvirtide.
Huber, KD; Little, SR; Rothstein, SN; Sluis-Cremer, N, 2014
)
0.93
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Env polyprotein Human immunodeficiency virus 1EC50 (µMol)0.18870.01010.18870.5420AID1161581; AID1161586; AID1161587
Env polyprotein Human immunodeficiency virus 1Kd0.18200.18200.18200.1820AID1197169
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (222)

Assay IDTitleYearJournalArticle
AID427598Antiviral activity against HIV1 Q23.71 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1161607Volume of distribution in rat at 4 mg/kg, iv administered as single dose2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID556146Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells in presence fresh human serum after 2 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1154160Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 Ba-L subtype B infected in human PBMC2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID1239321Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat Q40H mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
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SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
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AID1239340Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat N43K mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1161588Ratio of EC50 for HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/3 cells to CD4/CCR5 receptor expressing TZM-bl cells with wash out to EC50 for HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
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AID556150Antiviral activity against HIV1 harboring E57A mutant regulatory protein rev isolated from patient with viral infection assessed as change in viral RNA count after 48 weeks relative to control2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
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The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
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AID78755Anti-HIV activity was measured in H9-cells by fusion assay1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents.
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Bioassay-guided investigation of the Tanzanian plant Pyrenacantha kaurabassana for potential anti-HIV-active compounds.
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Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID1368354Antiviral activity against HIV-1 3B infected in human TZM-bl cells at 10 uM treated 2 to 6 hrs post infection for 2 hrs followed by compound washout measured after 2 days by luciferase reporter assay2018Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
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Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
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Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
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Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
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Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
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Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
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Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
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Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
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Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.
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Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID427779Antiviral activity against HIV1 RHPA4259.7 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID427778Antiviral activity against HIV1 TRO.11 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID1239329Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38M mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID556147Antiviral activity against HIV1 harboring wild type regulatory protein rev isolated from patient with viral infection assessed as viral RNA count after 48 weeks (Rvb = 4.9/ml)2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID499098Antiviral activity against HIV1 strain I-2496 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1161595Antiviral activity against T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A/N42D mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID647172Antiviral activity against HIV1 3B infected human TZM-bl cells assessed as inhibition of viral replication at 10 uM treated immediately after infection by luciferase reporter assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID509038Antiviral activity against HIV1 JRCSF infected in human vaginal epithelium leukocytes assessed as inhibition of viral genomic integration by titration assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID576517Antiviral activity against HIV-1 group O expressing gp41 T27A mutant gene2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID1056648Ratio of IC50 for enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38A mutation to IC50 for enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
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New approaches toward anti-HIV chemotherapy.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
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The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
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Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.
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The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID556154Antiviral activity against HIV1 harboring E57A mutant regulatory protein rev isolated from patient with viral infection assessed as change in CD4 cell count after 48 weeks relative to control2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID1808903Anti-HIV-1 activity against T20-resistant HIV1 V38E/N42S assessed as inhibition of infection in human CEMx174 5.25M7 cells expressing CCR5/CXCR4 by measuring P24 antigen after 6 days by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
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Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
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Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
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Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
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Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1056652Antiviral activity against enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)N42T/N43K mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID691717Antiviral activity against CCR5-tropic HIV1 NL-AD87 infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay2012Journal of natural products, Oct-26, Volume: 75, Issue:10
Bioassay-guided investigation of the Tanzanian plant Pyrenacantha kaurabassana for potential anti-HIV-active compounds.
AID406226Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication at 20 nM2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID328587Half life in cynomolgus monkey at 1 to 2 mg/kg, iv2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID328589Antiviral activity against HIV1 098 isolate infected in human PBMCs by reverse transcriptase assay2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID1056653Antiviral activity against enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38A mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
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Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID509030Antiviral activity against HIV1 JRCSF infected in human vaginal intraepithelial cells assessed as decrease in viral genomic integration at 0.223 uM by singleplex PCR assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID556144Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/I37K/N126K/L204I mutation and 5-amino-acid deletion in the V4 region of gp120 protein by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID509039Antiviral activity against HIV1 JRCSF infected in PHA-activated human T cells assessed as inhibition of viral genomic integration by titration assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID1161594Antiviral activity against T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1239317Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID406224Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication at 5 nM2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID427601Antiviral activity against HIV1 Q769.d22 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1161581Inhibition of HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/3 cells to CD4/CCR5 receptor expressing TZM-bl cells after 6 to 8 hrs by luciferase assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1239325Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38A/N42T double mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
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The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1161587Inhibition of HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/3 cells to CD4/CCR5 receptor expressing TZM-bl cells compound preincubated for 1 hr followed by wash out measured after 48 hrs by prime/wash assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1239318Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat I37T mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID328591Antiviral activity against HIV1 098-T1249 isolate infected in human PBMCs by reverse transcriptase assay2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID499101Antiviral activity against HIV1 ETH2220 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1239324Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat I37T/N43K double mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1816668Antiviral activity against HIV 1 JRFL subtype B assessed as inhibition of viral entry preincubated for 30 min followed by U87-CD4-CRC5 positive cells addition and culture medium replacement after 12 hrs post infection and measured after 48 hrs by lucifera2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Supercoiling Structure-Based Design of a Trimeric Coiled-Coil Peptide with High Potency against HIV-1 and Human β-Coronavirus Infection.
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Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
AID1239328Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38A mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1368347Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.
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Multimerized CHR-derived peptides as HIV-1 fusion inhibitors.
AID427602Antiviral activity against HIV1 Q259.d2.17 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1154163Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 02CM0015BBY subtype CRF02_AG infected in human PBMC2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID427789Antiviral activity against HIV1 CAP.2.00.G3 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1816670Antiviral activity against HIV 1 BaL(R5) incubated overnight by ELISA analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Supercoiling Structure-Based Design of a Trimeric Coiled-Coil Peptide with High Potency against HIV-1 and Human β-Coronavirus Infection.
AID499099Antiviral activity against HIV1 UG273 clade A, R5 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID555966Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/V38A mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID509041Antiviral activity against HIV1 JRCSF infected in human intraepithelial leukocytes assessed as decrease viral integration at 0.5 ug/ml by titration assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID427787Antiviral activity against HIV1 ZM55F.PB28a infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1239336Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat I37T mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1161602Ratio of EC50 for T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38E/N42S mutant infected in human MT2 cells to EC50 for T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1161599Ratio of EC50 for T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A mutant infected in human MT2 cells to EC50 for T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID556142Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N43D/S138A mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells relative to HIV1 NL4-3 gp41 D36G mutant2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID555964Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1239334Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38A/N42T double mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID328592Antiviral activity against HIV1 098-T651 isolate infected in human PBMCs by reverse transcriptase assay2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID427783Antiviral activity against HIV1 Du151.2 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID427785Antiviral activity against HIV1 ZM197M.PB7 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID427786Antiviral activity against HIV1 ZM214M.PL15 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1161597Antiviral activity against T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38E/N42S mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID556138Antiviral activity against Human immunodeficiency virus 1 NL4-3 assessed as decrease in EC50 by MAGI assay relative to ddC2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID647173Antiviral activity against HIV1 3B infected human TZM-bl cells assessed as inhibition of viral replication at 10 uM treated 2 hrs after viral infection by luciferase reporter assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID427792Cytotoxicity against human TZM-bl cells after 2 days by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID499102Antiviral activity against HIV1 DJ259 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1154150Antiviral activity against HIV-1 Ba-L subtype B infected in human PBMC assessed as reverse transcriptase activity after 6 days by microtiter plate-based assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID427606Antiviral activity against HIV1 5768.4 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1239330Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat Q40H mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1161593Antiviral activity against T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID427599Antiviral activity against HIV1 Q168.a2 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID427784Antiviral activity against HIV1 Du422.1 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1056655Antiviral activity against enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID427790Antiviral activity against HIV1 CAP244.2.00.D3 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID576513Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD)2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID1879947Antiviral activity against T20-sensitive HIV-1 D36G assessed as inhibition of viral replication measured after 4 days by ELISA2022European journal of medicinal chemistry, Jun-05, Volume: 236Design of artificial α-helical peptides targeting both gp41 deep pocket and subpocket as potent HIV-1 fusion inhibitors.
AID1161606Half life in rat at 4 mg/kg, iv at 4 mg/kg, iv administered as single dose2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1879944Antiviral activity against HIV-1 IIIB assessed as inhibition of viral replication measured after 4 days by ELISA2022European journal of medicinal chemistry, Jun-05, Volume: 236Design of artificial α-helical peptides targeting both gp41 deep pocket and subpocket as potent HIV-1 fusion inhibitors.
AID1161600Ratio of EC50 for T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A/N42D mutant infected in human MT2 cells to EC50 for T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1816669Antiviral activity against HIV-1 IIIB assessed as inhibition of HIV-1 Env mediated cell-cell fusion in MT-2 cells preincubated for 30 mins followed by cell addition and measured after 2 hrs by calcein AM staining based fluorescence microscopy2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Supercoiling Structure-Based Design of a Trimeric Coiled-Coil Peptide with High Potency against HIV-1 and Human β-Coronavirus Infection.
AID1239335Ratio of IC50 for wild type HIV1 NL4-3 to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID555968Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N43D/S138A mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1808902Anti-HIV-1 activity against T20-sensitive HIV1 D36G assessed as inhibition of infection in human CEMx174 5.25M7 cells expressing CCR5/CXCR4 by measuring P24 antigen after 6 days by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
AID1197170Binding affinity to HIV1 gp41 (46 residues) assessed as effect on protein secondary structure measured as alpha-helicity in PBS buffer at pH 7.2 by circular dichroism assay (Rvb = 117 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
AID406228Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID647166Cytotoxicity in human TZM-bl cells by MTT assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID427782Antiviral activity against HIV1 Du123.6 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID658682Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with HIV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 300 nM after 3 days by beta-galactosidase assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID1197171Plasma concentration in Sprague-Dawley rat at 1.7 umol/kg, sc after 6 hrs2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
AID556151Antiviral activity against HIV1 harboring wild type regulatory protein rev isolated from patient with viral infection assessed as CD4 cell count after 48 weeks (Rvb = 146/ul)2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID763717Antiviral activity against HIV1 NL4-3 assessed as inhibition of viral fusion with human TZM-bl cells after 48 hrs by steady glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Multimerized CHR-derived peptides as HIV-1 fusion inhibitors.
AID389175Binding affinity to HIV1 heptad repeat 1 peptide N36 assessed as melting temperature of drug-HR1 peptide complex2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Identification of minimal sequence for HIV-1 fusion inhibitors.
AID556153Antiviral activity against HIV1 harboring wild type regulatory protein rev isolated from patient with viral infection assessed as change in CD4 cell count after 48 weeks relative to control2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID1197167Antiviral activity against HIV-1 SF33 infected in TZM-bl cells after 2 days by luciferase reporter gene assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
AID1154153Antiviral activity against HIV-1 02CM0015BBY subtype CRF02_AG infected in human PBMC assessed as reverse transcriptase activity after 6 days by microtiter plate-based assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID556140Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/V38A mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells relative to HIV1 NL4-3 gp41 D36G mutant2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1161611Half life in rat kidney homogenate at 8 ug/ml2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID499100Antiviral activity against HIV1 US2 clade B, R5 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1161608Cmax in rat at 4 mg/kg, iv administered as single dose2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID328593Binding affinity to HIV1 gp41 heptad repeat 1 region assessed as thermal stability of HR1/HR2 peptide bundle complex at 10 uM in presence of 8M urea2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID658573Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with VSV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 300 nM after 3 days by beta-galactosidase assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID1056645Ratio of IC50 for enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38A/N42T mutation to IC50 for enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID1239322Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat N43K mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID556152Antiviral activity against HIV1 harboring E57A mutant regulatory protein rev isolated from patient with viral infection assessed as CD4 cell count after 48 weeks (Rvb = 176/ul)2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID1774091Antiviral activity against VSV envelope pseudotyped HIV infected in MT2 cells assessed as luminescence measured after 48 hrs by viral entry evaluation assay2021Journal of natural products, 10-22, Volume: 84, Issue:10
Withanolide-Type Steroids from
AID509042Antiviral activity against HIV1 JRCSF infected in human intraepithelial leukocytes assessed as decrease viral integration at 0.1 ug/ml by titration assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID1161582Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production by ELISA2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1239333Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat I37T/N43K double mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID427776Antiviral activity against HIV1 QH0515.1 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID389174Antiviral activity against HIV1 in human 293T cells assessed as inhibition of viral replication after 48 hrs by multinuclear activation of galactosidase indicator assay2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Identification of minimal sequence for HIV-1 fusion inhibitors.
AID1161609Half life in rat liver homogenate at 8 ug/ml2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID406215Antiviral activity against HIV1 ADA in human PBMC assessed as reduction of p24 antigen levels2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID499095Antiviral activity against HIV1 NL4.3 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1239320Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38M mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID499094Antiviral activity against HIV1 3B/LA1 infected in HUT-78 cells co-cultured with uninfected human SupT1 CD4+ T-cell assessed as inhibition of envelope mediated cell-cell fusion after 16-20 hrs by cell-cell fusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID499096Antiviral activity against HIV1 Ba-L in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID499106Elimination half life in Wister rat at 4 mg/ kg, iv2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1056651Antiviral activity against enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38E/N42S mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID556141Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N43D mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells relative to HIV1 NL4-3 gp41 D36G mutant2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID499104Cytotoxicity against human CEM cells up to 100 uM by MTS assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID556148Antiviral activity against HIV1 harboring E57A mutant regulatory protein rev isolated from patient with viral infection assessed as viral RNA count after 48 weeks (Rvb = 4.9/ml)2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID556143Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N126K mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells relative to HIV1 NL4-3 gp41 D36G mutant2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1161601Ratio of EC50 for T20-resistant HIV1 NL4-3 harboring gp41 D36G/N42T/N43K mutant infected in human MT2 cells to EC50 for T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID576512Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE)2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID1056649Ratio of IC50 for enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38A/N42D mutation to IC50 for enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID1161605Mean residence time in rat at 4 mg/kg, iv administered as single dose2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1056646Ratio of IC50 for enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38E/N42S mutation to IC50 for enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID1161586Inhibition of HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/3 cells to CD4/CCR5 receptor expressing TZM-bl cells compound preincubated for 1 hr measured after 48 hrs by prime/wash assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID406227Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication at 40 nM2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID1056654Antiviral activity against enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38A/N42D mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID1056647Ratio of IC50 for enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)N42T/N43K mutation to IC50 for enfuvirtide-sensitive HIV-1 NL4-3 harboring gp41 (36G)N42S mutation2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
AID647168Binding affinity to human serum albumin by fluorescence quenching assay2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Synthesis and antiviral activities of novel gossypol derivatives.
AID555967Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N43D mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID576518Antiviral activity against HIV-1 group O expressing gp41 E119Q mutant gene2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID1154166Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 92UG001 subtype D infected in human PBMC2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID427791Cytotoxicity against human TZM-bl cells at 15 uM after 2 days by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1154159Cytotoxicity against human PBMC assessed as inhibition of cell viability by MTS assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID1239343Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38A/N42T double mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1161584Antiviral activity against HIV1 BaL infected in human MT2 cells assessed as inhibition of viral replication2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1239332Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36S/V38M double mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID499097Antiviral activity against HIV1 BZ167 in human PBMC assessed as p24 antigen level by ELISA2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1879953Selectivity ratio of EC50 for antiviral activity against T20-resistant HIV-1 V38A/N42T to EC50 for antiviral activity against T20-sensitive HIV-1 D36G2022European journal of medicinal chemistry, Jun-05, Volume: 236Design of artificial α-helical peptides targeting both gp41 deep pocket and subpocket as potent HIV-1 fusion inhibitors.
AID1161583Cytotoxicity against human MT2 cells after 4 days by XTT assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1808904Anti-HIV-1 activity against T20 resistant HIV1 N427/N43K assessed as inhibition of infection in human CEMx174 5.25M7 cells expressing CCR5/CXCR4 by measuring P24 antigen after 6 days by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
AID427603Antiviral activity against HIV1 Q842.d12 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID1816667Antiviral activity against HIV 1 25710-2 subtype C assessed as inhibition of viral entry preincubated for 30 min followed by U87-CD4-CRC5 positive cells addition and culture medium replacement after 12 hrs post infection and measured after 48 hrs by lucif2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Supercoiling Structure-Based Design of a Trimeric Coiled-Coil Peptide with High Potency against HIV-1 and Human β-Coronavirus Infection.
AID427600Antiviral activity against HIV1 Q461.e2 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID509044Antiviral activity against HIV1 JRCSF infected in human vaginal epithelium mucosa assessed as decrease viral integration at 10 ng/ml by titration assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells.
AID1161596Antiviral activity against T20-resistant HIV1 NL4-3 harboring gp41 D36G/N42T/N43K mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID427780Antiviral activity against HIV1 REJO4541.67 infected in human TZM-b1 cells assessed as inhibition of viral infection after 2 days postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
AID425894Antiviral activity against HIV1 3B infected human MT2 cells assessed as cytoprotection after 5 days by MTT colorimetric method2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Identification of a beta3-peptide HIV fusion inhibitor with improved potency in live cells.
AID328586Clearance in cynomolgus monkey at 1 to 2 mg/kg, iv2007Proceedings of the National Academy of Sciences of the United States of America, Jul-31, Volume: 104, Issue:31
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
AID1239338Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat V38M mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1239339Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat Q40H mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1816671Antiviral activity against HIV 1 IIIB(X5) incubated overnight by ELISA analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Supercoiling Structure-Based Design of a Trimeric Coiled-Coil Peptide with High Potency against HIV-1 and Human β-Coronavirus Infection.
AID576514Antiviral activity against HIV-1 group O2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
AID1239327Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat I37T mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1161598Antiviral activity against T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A/N42T mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1161604AUC (0 to t) in rat at 4 mg/kg, iv administered as single dose2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID1808905Anti-HIV-1 activity against T20 resistant HIV1 V38A/N427 assessed as inhibition of infection in human CEMx174 5.25M7 cells expressing CCR5/CXCR4 by measuring P24 antigen after 6 days by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
AID406225Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication at 10 nM2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
AID1161603Ratio of EC50 for T20-resistant HIV1 NL4-3 harboring gp41 D36G/V38A/N42T mutant infected in human MT2 cells to EC50 for T20-sensitive HIV1 NL4-3 harboring gp41 D36G mutant infected in human MT2 cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.
AID556137Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/I37K/N126K/L204I mutation and 5-amino-acid deletion in the V4 region of gp120 protein by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID499092Antiviral activity against HIV1 3B/LA1 infected in human CD4+ T-cell assessed as inhibition of giant cell formation2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
AID1879948Antiviral activity against T20-resistant HIV-1 V38E/N42S assessed as inhibition of viral replication measured after 4 days by ELISA2022European journal of medicinal chemistry, Jun-05, Volume: 236Design of artificial α-helical peptides targeting both gp41 deep pocket and subpocket as potent HIV-1 fusion inhibitors.
AID1239341Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36S/V38M double mutant to IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36G mutant2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID555969Antiviral activity against enfuvirtide-resistant Human immunodeficiency virus 1 NL4-3 harboring gp41 D36G/N126K mutation by MAGI assay using human HeLa Cd4/LTR-beta-galactosidase cells2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
AID1239331Ratio of IC50 for ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat N43K mutant to IC50 for wild type HIV1 NL4-32015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
AID1154165Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 00UG_D26830M4 subtype D infected in human PBMC2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.
AID556149Antiviral activity against HIV1 harboring wild type regulatory protein rev isolated from patient with viral infection assessed as change in viral RNA count after 48 weeks relative to control2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Treatment with the fusion inhibitor enfuvirtide influences the appearance of mutations in the human immunodeficiency virus type 1 regulatory protein rev.
AID1239323Antiviral activity against ENF-resistant HIV1 NL4-3 harboring gp41 N-terminal heptad repeat D36S/V38M double mutant infected in human TZM-bl cells assessed as inhibition of viral entry into cells after 48 hrs by single-cycle infection assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (660)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's27 (4.09)18.2507
2000's446 (67.58)29.6817
2010's170 (25.76)24.3611
2020's17 (2.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index57.50 (24.57)
Research Supply Index6.69 (2.92)
Research Growth Index5.51 (4.65)
Search Engine Demand Index95.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (57.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials89 (12.40%)5.53%
Reviews90 (12.53%)6.00%
Case Studies45 (6.27%)4.05%
Observational0 (0.00%)0.25%
Other494 (68.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (39)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multicenter, Open-label Study Evaluating the Safety and Efficacy of a New Protease Inhibitor (Darunavir) With Fuzeon® (Enfuvirtide) Plus Background Antiretroviral Regimen in HIV-1 Infected, Triple-class Treatment-experienced Patients [NCT00326963]Phase 4142 participants (Actual)Interventional2006-03-31Completed
A Phase I/II Pharmacokinetic and Safety Study of T-20 in Combination With an Optimized Background in HIV Infected Children and Adolescents [NCT00022763]Phase 252 participants (Actual)Interventional2001-08-31Completed
Optimized Antiretroviral Therapy During Allogeneic Hematopoietic Stem Cell Transplantation in HIV-1-infected Individuals [NCT01836068]Early Phase 111 participants (Actual)Interventional2013-06-30Completed
A Randomized, Open-label Study Evaluating the Antiviral Activity and Safety of 3 Month Fuzeon Induction With an Optimized Background Antiretroviral Regimen Versus OB Alone, in Fuzeon-naive HIV-1 Infected Patients With Virological Failure. [NCT00615134]Phase 229 participants (Actual)Interventional2008-01-31Completed
SPRING: Safety, Efficacy, Pharmacokinetics of tipRanavi/r IN Race/Gender HIV+ Patients Randomized to Therapeutic Drug Monitoring or Standard of Care [NCT00440271]Phase 333 participants (Actual)Interventional2007-02-28Terminated
Phase IIIb/IV Randomized, Controlled Study Evaluating an Intensification Treatment Strategy of Adding Enfuvirtide (ENF) to an Oral Highly Active AntiRetroviral Therapy (HAART) in Treatment Experienced Patients [NCT00487188]Phase 447 participants (Actual)Interventional2005-11-30Completed
Effect of Enfuvirtide on Lipid and Glucose Metabolism and Mitochondrial Function in Healthy Volunteers [NCT00657761]Phase 415 participants (Actual)Interventional2005-09-30Completed
The Optimized Treatment That Includes or Omits NRTIs Trial: A Randomized Strategy Study for HIV-1-Infected Treatment-Experienced Subjects Using the cPSS to Select an Effective Regimen [NCT00537394]Phase 3517 participants (Actual)Interventional2008-01-31Completed
An Open-Label Trial With TMC125 in HIV-1 Infected Subjects, Who Were Randomized to a TMC125 Treatment Arm in a Sponsor-Selected TMC125 Trial and Were Treated for at Least 48 Weeks [NCT00128830]Phase 2211 participants (Actual)Interventional2005-06-30Completed
An Open-label Study of a HAART (Highly Active Antiretroviral Therapy) Regimen Containing Subcutaneous Injection of Fuzeon on Quality of Life in Clinically Stable, Treatment-experienced Patients With HIV-1 Infection [NCT00232908]Phase 4361 participants (Actual)Interventional2004-06-30Completed
An Open-label Study of the Tolerability of a Subcutaneous Needle-free Injection Device Used to Administer Fuzeon, Compared With the Standard Needle/Syringe Supplied With Commercial Fuzeon in HIV-1 Infected, ARV Treatment-experienced Adults [NCT00233883]Phase 458 participants (Actual)Interventional2005-08-31Completed
The Radata-Fuzeon Cohort - An Observational Cohort-Study in HIV-Infected Patients Using Fuzeon (Enfuvirtide) as Part of Their Antiretroviral Combination Therapy [NCT00216359]200 participants Observational2003-05-31Active, not recruiting
Open Label, Nonrandomized Clinical Trial of Safety and Tolerability of Enfuviritide (Fuzeon®, HIV Fusion Inhibitor) in Patients With Advanced HIV1 Infection [NCT02569502]Phase 46 participants (Actual)Interventional2005-04-30Completed
Open-label, Randomised and Multi-center Study Evaluating the Efficacy and Safety of an Optimised Background Antiretroviral Regimen (OB) Compared to OB Associated With Enfuvirtide in Previously Treated HIV-1 Infected Patients in Virological Success After a [NCT02733419]Phase 384 participants (Actual)Interventional2004-12-31Completed
Biojector 2000 Open-Label Safety Study (BOSS) to Evaluate Signs and Symptoms Associated With a Needle-free Injection Device for Administration of Fuzeon to Patients With HIV-1 Infection [NCT00337701]Phase 4326 participants (Actual)Interventional2006-06-30Completed
A Pilot Randomized Controlled Trial of Adding Enfuvirtide to Standard Combination Antiretroviral Therapy in HIV-infected Individuals With Full Virologic Suppression to Further Suppress Proviral HIV DNA [NCT00334022]18 participants (Actual)Interventional2006-02-28Completed
Analysis of Lipodystrophy in HIV-Infected Individuals A Prospective, Non-randomised, 48 Week Study of the Effect of PI Containing and Non-PI Containing Antiretroviral Regimens on the Expression of Adipocyte Specific Genes, Protein Levels and Cellular Stru [NCT00192660]Phase 480 participants (Actual)Interventional2003-02-28Completed
An Open-label, Randomized, Cross-over Study in HIV-Positive Subjects to Determine and Compare the Single-dose Pharmacokinetics of Enfuvirtide after a Single 90 mg SC Administration [NCT00086710]Phase 126 participants InterventionalCompleted
Partial Treatment Interruptions in HIV-1 Patients With Multi-Drug Resistant Virus [NCT00187551]Phase 425 participants (Actual)Interventional2000-05-31Completed
A Randomized Phase I/II Placebo-controlled Study of Amdoxovir (DAPD) Versus Placebo Together With Enfuvirtide (T-20) Plus Optimized Background Therapy for HIV-Infected Subjects Failing Current Therapy [NCT00031044]Phase 1/Phase 250 participants InterventionalCompleted
A Phase II Open-label, Randomized, Active-controlled Study Comparing the Efficacy and Safety of Once Daily Enfuvirtide Dosing Versus the Currently Recommended Twice Daily Dosing in HIV-1 Infected Treatment-experienced Patients. [NCT00089492]Phase 264 participants (Actual)Interventional2004-07-31Completed
A Randomized, Open Label Study to Determine the Immunological Benefits of Adding Fuzeon to an Antiretroviral Regimen in HIV-infected Fuzeon-naïve Patients With Sustained HIV Viral Suppression [NCT00461266]Phase 40 participants (Actual)Interventional2007-04-30Withdrawn(stopped due to Slow recruitment)
Prospective Clinical Trial to Assess Safety and Efficacy of DRV/r(TMC 114/r), ETV(TMC 125) and MK-0518 in Addition to OBT in HIV-1 Infected Patients With Limited to No Treatment Options ANRS 139 TRIO [NCT00460382]Phase 2103 participants (Actual)Interventional2007-05-31Completed
[NCT00100984]Phase 48 participants (Actual)Interventional2004-07-21Terminated(stopped due to Insufficient enrollment)
Treatment Intensification in HIV-1 Patients With Multi-Drug Resistant Virus [NCT00102934]20 participants (Actual)Interventional2003-03-31Active, not recruiting
A Phase III Open-Label, Randomized, Active-Controlled Study Assessing the Efficacy and Safety of T-20 (HIV-1 Fusion Inhibitor) in Combination With an Optimized Background Regimen, Versus Optimized Background Therapy Alone, in Patients With Prior Experienc [NCT00008528]Phase 3525 participants InterventionalCompleted
Early Intensification of Combination Antiretroviral Therapy Including FUZEON® in the Treatment of Progressive Multifocal Leucoencephalopathy During HIV-1 Infection ANRS 125 Trial [NCT00120367]Phase 230 participants Interventional2005-04-30Completed
A Phase I/II Study of T-20, a Fusion Inhibitor, in HIV-1 Infected Children [NCT00001118]Phase 124 participants InterventionalCompleted
A Phase III Open-Label, Randomized, Active-Controlled Study Assessing the Efficacy and Safety of T-20 (HIV-1 Fusion Inhibitor) in Combination With an Optimized Background Regimen, Versus Optimized Background Regimen Alone, in Patients With Prior Experienc [NCT00021554]Phase 3525 participants InterventionalCompleted
Multicenter, Open-Label, Early Acces Program of Fuzeon (Enfuvirtide T-20/Ro 29,9800, HIV-1 Fusion Inhibitor) in Combination With Free Choice Antiretroviral Regimen to Assess Serious Adverse Events, Serious AIDS-Defining Events, and Tolerability in Patient [NCT00050856]Phase 35 participants Interventional2002-11-30Completed
A Pilot Study to Measure the Clearance of Replication-Competent HIV-1 in Resting Memory CD4+ Cells in HIV-1-Infected Subjects Who Receive Enfuvirtide Plus Oral Combination Antiretroviral Therapy [NCT00051831]19 participants (Actual)Interventional2003-10-31Completed
A Multicenter, Open-label Study Evaluating the Antiviral Activity and Safety of Enfuvirtide (ENF) Once Daily (QD) or Twice Daily (BID) in Triple-class Experienced HIV-1 Infected Patients Changing Their Therapy to a Standard of Care (SOC) Regimen That Incl [NCT00488059]Phase 429 participants (Actual)Interventional2007-06-30Terminated(stopped due to This study was terminated early due to poor enrollment.)
Inhibiting Histone Deacetylase: Toward Eradication of HIV [NCT00312546]Phase 114 participants (Actual)Interventional2006-06-30Terminated
Enfuvirtide for the Initial Phase of Antiretroviral Therapy in HIV-infected Patients With High Risk of Clinical Progression : ANRS 130 APOLLO [NCT00302822]Phase 3195 participants (Actual)Interventional2006-04-30Completed
Viral Decay Kinetics During Induction Therapy With or Without the Use of Enfuvirtide in HAART-naÃ-ve Patients With Advanced HIV [NCT00344760]Phase 42 participants (Anticipated)Interventional2005-01-31Completed
An Open-Label Safety Trial of Enfuvirtide (T-20/RO 29-9800, HIV-1 Fusion Inhibitor) in Combination With Free Choice Antiviral Regimen in Thai Patients With Advanced HIV Infection [NCT02582983]Phase 423 participants (Actual)Interventional2004-02-29Completed
A Phase II Evaluation of the Safety, Plasma Pharmacokinetics, and Antiviral Activity of T-20 Administered to HIV-1 Positive Adults By Continuous Subcutaneous Infusion or Subcutaneous Injection [NCT00002228]Phase 278 participants InterventionalCompleted
A Controlled Phase 2 Trial Assessing Three Doses of T-20 in Combination With Abacavir, Amprenavir, Ritonavir, and Efavirenz in HIV-1 Infected Adults [NCT00002239]Phase 268 participants Interventional1999-05-31Completed
Randomized Clinical Trial to Evaluate the Interest of a Down-scaled Treatment Strategy Using Dual Therapy (Nucleoside Analogs) in HIV Infected Patients Already Being Treated Using Triple Therapy, Who Present With a Successful Virological Control and for W [NCT02302547]Phase 3224 participants (Actual)Interventional2014-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00022763 (10) [back to overview]Number of Participants Who Died
NCT00022763 (10) [back to overview]Time to Maximum Plasma Concentration (Tmax) for Enfuvirtide
NCT00022763 (10) [back to overview]Area Under the Plasma Concentration Time Curve (AUC) From 0-12 Hours for Enfuvirtide and Its Metabolite (Ro 50-6343)
NCT00022763 (10) [back to overview]Maximum Plasma Concentration (Cmax) for Enfuvirtide and Its Metabolite (Ro 50-6343)
NCT00022763 (10) [back to overview]Minimum Plasma Concentration (Ctrough) for Enfuvirtide and Its Metabolite (Ro 50-6343)
NCT00022763 (10) [back to overview]Number of Participants With Adverse Events (AEs) and Serious AEs
NCT00022763 (10) [back to overview]Number of Participants With Treatment Emergent Grade 3 or Grade 4 Laboratory Abnormalities
NCT00022763 (10) [back to overview]Number of Participants With Worst Local Injection Site Reactions
NCT00022763 (10) [back to overview]AUC12h Ratio of Enfuvirtide Metabolite (Ro 50-6343)/ENF (Ro 29-9800)
NCT00022763 (10) [back to overview]Number of Participants Who Prematurely Withdrew Due to AE
NCT00128830 (10) [back to overview]Median Change From TMC125-C229 Baseline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 96
NCT00128830 (10) [back to overview]Number of Participants With Emerging Mutation (Reverse Transcriptase Mutation)
NCT00128830 (10) [back to overview]Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Viral Load Less Than 400 Copies/mL; and Greater Than or Equal to 1 log10 Decrease From Baseline) at Week 192
NCT00128830 (10) [back to overview]Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Less Than 400 Copies/mL; and Greater Than or Equal to 1 Log 10 Decrease From Baseline) at Week 96
NCT00128830 (10) [back to overview]Number of Participants With Adverse Events
NCT00128830 (10) [back to overview]Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 96
NCT00128830 (10) [back to overview]Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 48
NCT00128830 (10) [back to overview]Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 96
NCT00128830 (10) [back to overview]Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 192
NCT00128830 (10) [back to overview]Median Change From TMC125-C229 Basline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 48
NCT00326963 (17) [back to overview]Percentage of Participants With 1 or More Injection Site Reactions Meeting the Criteria of an Serious Adverse Event
NCT00326963 (17) [back to overview]Change From Baseline in CD4+ Lymphocyte Count
NCT00326963 (17) [back to overview]Change From Baseline in Log 10 Plasma HIV-1 RNA Viral Load
NCT00326963 (17) [back to overview]Descriptive Summary of ISR Parameters (ie, Severity and Frequency of Pain and Symptoms) by Injection Device Based on an ISR Grading Tool.
NCT00326963 (17) [back to overview]Number of Participants Adhering to Enfuvirtide (ENF)
NCT00326963 (17) [back to overview]Number of Participants Discontinuing Study Medication Due to Clinical Adverse Events
NCT00326963 (17) [back to overview]Number of Participants Meeting Virologic Failure Criteria
NCT00326963 (17) [back to overview]Number of Participants With Any Adverse Event (AE) and Serious Adverse Event (SAE)
NCT00326963 (17) [back to overview]Number of Participants With HIV-1 RNA Viral Load <50 Copies/mL
NCT00326963 (17) [back to overview]Number of Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Viral Load <50 Copies/mL
NCT00326963 (17) [back to overview]Percentage of Participants Adhering to ENF
NCT00326963 (17) [back to overview]Percentage of Participants Meeting Virologic Failure Criteria
NCT00326963 (17) [back to overview]Percentage of Participants With HIV-1 RNA Viral Load <400 Copies/mL
NCT00326963 (17) [back to overview]Percentage of Participants With HIV-1 RNA Viral Load <50 Copies/mL
NCT00326963 (17) [back to overview]Percentage of Participants With HIV-1 RNA Viral Load <50 Copies/mL
NCT00326963 (17) [back to overview]Number of Participants With HIV-1 RNA Viral Load <400 Copies/mL
NCT00326963 (17) [back to overview]Number of Participants With 1 or More Injection Site Reactions Meeting the Criteria of an Serious Adverse Event
NCT00487188 (14) [back to overview]Change From Baseline to Week 24 in Cluster Differentiation Antigen Four Positive (CD4+) Cell Counts
NCT00487188 (14) [back to overview]Number of Participants With Adverse Events (AEs) During the Induction Phase
NCT00487188 (14) [back to overview]Percentage of Participants Maintaining CD4+ Count During the Maintenance Phase
NCT00487188 (14) [back to overview]Percentage of Participants With Improvement in CD4+ Count During the Maintenance Phase
NCT00487188 (14) [back to overview]Number of Participants With Viral Suppression: HIV-1 RNA < 50 Copies/mL During the Induction Phase
NCT00487188 (14) [back to overview]Number of Participants With Viral Suppression HIV-1 RNA < 400 Copies/mL During the Induction Phase
NCT00487188 (14) [back to overview]Change From Baseline to Week 48 in Cluster Differentiation Antigen Four Positive (CD4) Cell Counts
NCT00487188 (14) [back to overview]Change From Baseline to Week 24 in Viral Load
NCT00487188 (14) [back to overview]Time to Virological Failure During the Maintenance Phase
NCT00487188 (14) [back to overview]Time to Loss of Viral Response During the Maintenance Phase
NCT00487188 (14) [back to overview]Time to Achieving HIV-1 RNA < 50 Copies/mL During the Induction Phase
NCT00487188 (14) [back to overview]Percentage of Maintenance Phase Participants With Viral Load < 50 Copies/mL at 48 Weeks
NCT00487188 (14) [back to overview]Percentage of Induction Phase Participants With Viral Load < 50 Copies/mL at 48 Weeks
NCT00487188 (14) [back to overview]Number of Participants With Virological Failure During the Maintenance Phase
NCT00488059 (7) [back to overview]Number of Patients in Phase II of the Study With HIV-1 RNA ≤ 50 Copies/mL at Week II-16
NCT00488059 (7) [back to overview]CD4+ Lymphocyte Count Change From Baseline
NCT00488059 (7) [back to overview]HIV-1 RNA Viral Load Change From Baseline in Phase I of the Study
NCT00488059 (7) [back to overview]Number of Patients in Phase I of the Study With a Confirmed HIV-1 RNA Viral Load ≤ 50 Copies/mL
NCT00488059 (7) [back to overview]Percentage of Patients With Ongoing Injection Site Reactions (ISRs)
NCT00488059 (7) [back to overview]Virologic Response Over Time in Phase I of the Study
NCT00488059 (7) [back to overview]Virologic Response Over Time in Phase II of the Study
NCT00537394 (15) [back to overview]Change in Plasma HIV-1 Viral Load From Baseline to Week 1
NCT00537394 (15) [back to overview]Number of Participants With Change in Virus Co-receptor Tropism Among Those With R5-only Tropic Virus at Study Entry
NCT00537394 (15) [back to overview]Participants With Newly Acquired HIV Drug Resistance Between Study Entry and Confirmed Virologic Failure
NCT00537394 (15) [back to overview]Percent of Participants With Regimen Failure, Defined as a Confirmed Virologic Failure or Discontinuation of Randomized NRTI Component of Study Treatment
NCT00537394 (15) [back to overview]Change in Cardiovascular Risk Score From Baseline
NCT00537394 (15) [back to overview]Change in CD4 Count From Baseline
NCT00537394 (15) [back to overview]Change in Fasting Non-HDL Cholesterol From Baseline
NCT00537394 (15) [back to overview]Change in Summarized Quality of Life Score
NCT00537394 (15) [back to overview]Number of Participants Self-reporting Non-adherence to Assigned Study ARVS (Excluding NRTIs, if Applicable)
NCT00537394 (15) [back to overview]Number of Participants With Plasma HIV-1 Viral Load < 50 Copies/ml
NCT00537394 (15) [back to overview]Time From Randomization to Confirmed Virological Failure
NCT00537394 (15) [back to overview]Time From Randomization to Discontinuation of Randomized NRTI Component of Study Treatment
NCT00537394 (15) [back to overview]Time From Treatment Dispensation to First Grade 3 or Higher (and at Least One Grade Higher Than Baseline) Signs/Symptom or Laboratory Abnormality
NCT00537394 (15) [back to overview]Time From Treatment Dispensation to First Study ARV Modification (Excluding NRTIs, if Applicable)
NCT00537394 (15) [back to overview]Time From Treatment Dispensation to Serious Non-AIDS-defining Events
NCT02582983 (2) [back to overview]Number of Participants With Premature Withdrawal Due to Adverse Events
NCT02582983 (2) [back to overview]Number of Participants With Serious Adverse Events (SAEs)

Number of Participants Who Died

(NCT00022763)
Timeframe: Up to Week 96

Interventionparticipants (Number)
Stratum A1
Stratum B1

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Time to Maximum Plasma Concentration (Tmax) for Enfuvirtide

Tmax is defined as actual sampling time to reach maximum observed analyte concentration. (NCT00022763)
Timeframe: Pre-dose (time 0), and 2, 4, 8, and 12 hours post-dose (Week 1)

Interventionhour (Mean)
Stratum A4.13
Stratum B5.05

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Area Under the Plasma Concentration Time Curve (AUC) From 0-12 Hours for Enfuvirtide and Its Metabolite (Ro 50-6343)

The Area Under the Plasma Concentration-Time Curve (AUC) is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. AUC was calculated from plasma concentration-time data (on Day 7) using standard non-compartmental pharmacokinetic methods. (NCT00022763)
Timeframe: Pre-dose (time 0), and 2, 4, 8, and 12 hours post-dose (Week 1)

,
Interventionmicrogram hour per milliliter (mcg.h/mL) (Mean)
EnfuvirtideMetabolite (Ro 50-6343)
Stratum A56.13.07
Stratum B52.73.41

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Maximum Plasma Concentration (Cmax) for Enfuvirtide and Its Metabolite (Ro 50-6343)

The Plasma Concentration (Cmax) is defined as maximum observed analyte concentration. Cmax was calculated from plasma concentration-time data (on Day 7) using standard non-compartmental pharmacokinetic methods. (NCT00022763)
Timeframe: Pre-dose (time 0), and 2, 4, 8, and 12 hours post-dose (Week 1)

,
Interventionmcg/mL (Mean)
EnfuvirtideMetabolite (Ro 50-6343)
Stratum A6.430.434
Stratum B5.880.450

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Minimum Plasma Concentration (Ctrough) for Enfuvirtide and Its Metabolite (Ro 50-6343)

Ctrough is defined as the lowest concentration that a drug reaches before the next dose is administered. (NCT00022763)
Timeframe: Pre-dose (time 0), and 2, 4, 8, and 12 hours post-dose (Week 1)

,
Interventionmcg/mL (Mean)
EnfuvirtideMetabolite (Ro 50-6343)
Stratum A2.870.177
Stratum B2.980.242

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Number of Participants With Adverse Events (AEs) and Serious AEs

An AE is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is a significant medical event. (NCT00022763)
Timeframe: Up to Week 4 after discontinuation of therapy

,
Interventionparticipants (Number)
Any AEAny SAE
Stratum A248
Stratum B2515

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Number of Participants With Treatment Emergent Grade 3 or Grade 4 Laboratory Abnormalities

Pediatric AIDS Clinical Trials Group (PACTG) toxicity grading scale was used for reviewing and grading clinically significant laboratory abnormalities. PACTG Grade 3 and Grade 4 were considered Severe and life threatening, respectively. (NCT00022763)
Timeframe: Up to Week 96

,
Interventionparticipants (Number)
Platelets Grade 3Platelets Grade 4Neutrophils Grade 3Neutrophils Grade 4ASAT Grade 3ASAT Grade 4ALAT Grade 3ALAT Grade 4Total Bilirubin Grade 3Total Bilirubin Grade 4GGT Grade 3GGT Grade 4Amylase Grade 3Amylase Grade 4
Stratum A01012010000011
Stratum B20000000101011

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Number of Participants With Worst Local Injection Site Reactions

Numbers of Participants With worst local injection site reactions were reported. Localized injection site reactions like erythema, induration, pruritus, nodule and cyst, and ecchymosis were recorded. (NCT00022763)
Timeframe: Up to Week 96

,
Interventionparticipants (Number)
ErythemaNodules and CystsIndurationPruritusEcchymosisOthers
Stratum A1316211065
Stratum B1914209810

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AUC12h Ratio of Enfuvirtide Metabolite (Ro 50-6343)/ENF (Ro 29-9800)

The ratio of the area under plasma concentration-time curve from time 0 to 12 hours of Enfuvirtide Metabolite (Ro 50-6343) versus enfuvirtide was calculated. (NCT00022763)
Timeframe: Pre-dose (time 0), and 2, 4, 8, and 12 hours post-dose (Week 1)

InterventionRatio (Mean)
Stratum A5.31
Stratum B7.12

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Number of Participants Who Prematurely Withdrew Due to AE

(NCT00022763)
Timeframe: Up to Week 96

Interventionparticipants (Number)
Stratum A9
Stratum B17

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Median Change From TMC125-C229 Baseline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 96

The last visit of the TMC125 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies) was considered to be the TMC125-C229 baseline. (NCT00128830)
Timeframe: Week 96

Interventionx 1000000 cells/L (Median)
Etravirine18.50

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Number of Participants With Emerging Mutation (Reverse Transcriptase Mutation)

Emerging mutations are the mutation which are not present at baseline (last visit of the TMC125 feeder study [TMC125-C203 (NCT00412646), TMC125-C223 (NCT00081978), TMC125 C211 (NCT00111280) or TMC125-C209 feeder studies]) and are present at endpoint (last available timepoint during treatment period for each individual participant). (NCT00128830)
Timeframe: Baseline and Endpoint (ie, the last available time point during the treatment period)

InterventionParticipants (Number)
L100IY181CA98GV179IK103NH221Y
Etravirine876655

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Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Viral Load Less Than 400 Copies/mL; and Greater Than or Equal to 1 log10 Decrease From Baseline) at Week 192

Baseline considered for this outcome is the baseline in the respective TMC125-C229 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies). (NCT00128830)
Timeframe: Week 192

InterventionParticipants (Number)
Viral load (VL) less than 50 copies/mLVL less than 400 copies/mLVL greater than or equal to 1log10
Etravirine698183

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Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Less Than 400 Copies/mL; and Greater Than or Equal to 1 Log 10 Decrease From Baseline) at Week 96

Baseline considered for this outcome is the baseline in the respective TMC125-C229 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies). (NCT00128830)
Timeframe: Week 96

InterventionParticipants (Number)
Viral load (VL) less than 50 copies/mLViral load less than 400 copies/mLViral load more than or equal to 1log10
Etravirine105124132

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Number of Participants With Adverse Events

Number of participants who reported at least 1 of the adverse events. (NCT00128830)
Timeframe: Up to 3 years

InterventionParticipants (Number)
Etravirine195

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Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 96

Number of participants who had viral load more than or equal to 50 copies/mL and less than 50 copies/mL at TMC125-C229 baseline and who achieved virologic response (ie, viral load less than 50 copies/mL) at Week 96. The last visit of the TMC125 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies) was considered to be the TMC125-C229 baseline. (NCT00128830)
Timeframe: Week 96

InterventionParticipants (Number)
Viral Load More Than or Equal to 50 Copies/mL28
Viral Load Less Than 50 Copies/mL72

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Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 48

Number of participants who had viral load more than or equal to 50 copies/mL and less than 50 copies/mL at TMC125-C229 baseline and who achieved virologic response (ie, viral load less than 50 copies/mL) at Week 48. The last visit of the TMC125 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies) was considered to be the TMC125-C229 baseline. (NCT00128830)
Timeframe: Week 48

InterventionParticipants (Number)
Viral Load More Than or Equal to 50 Copies/mL22
Viral Load Less Than 50 Copies/mL80

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Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 96

Baseline considered for this outcome is the baseline in the respective TMC125-C229 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies). (NCT00128830)
Timeframe: Week 96

Interventionx 1000000 cells/mL (Median)
Etravirine120.00

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Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 192

Baseline considered for this outcome is the baseline in the respective TMC125-C229 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies). (NCT00128830)
Timeframe: Week 192

Interventionx 1000000 cells/mL (Median)
Etravirine149.50

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Median Change From TMC125-C229 Basline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 48

The last visit of the TMC125 feeder study (TMC125-C203 [NCT00412646], TMC125-C223 [NCT00081978], TMC125 C211 [NCT00111280] or TMC125-C209 feeder studies) was considered to be the TMC125-C229 baseline. (NCT00128830)
Timeframe: Week 48

Interventionx 100000 cells/L (Median)
Etravirine21.50

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Percentage of Participants With 1 or More Injection Site Reactions Meeting the Criteria of an Serious Adverse Event

Injection site reactions (ISRs) referred to any localized sign or symptom, including erythema, induration, pruritus, nodules, ecchymosis (degree of bruising/ discoloration), and pain/discomfort. Injection site reactions were monitored by trained study personnel at weeks 1, 4, 12, 16, and 24. Interruption of ENF for toxicity management of recurrent local grade 3 or 4 ISRs until the sign or symptom resolved to grade 2 was at the discretion of the investigator. Any individual injection site signs or symptoms meeting the criteria for a serious adverse event (SAE) had to be reported as an SAE. In the event of a serious ISR, the participant was to immediately discontinue ENF and withdraw from the study. If the participant was not already hospitalized, serious ISRs required a clinic visit within 72 hours of the event. (NCT00326963)
Timeframe: Week 1 to Week 24

InterventionPercentage of participants (Number)
Enfuvirtide+PI+ARV's0

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Change From Baseline in CD4+ Lymphocyte Count

Summary statistics for change from baseline in CD4+ lymphocyte count were presented . Change from baseline in CD4+ lymphocyte count was derived as follows: Change from baseline = (CD4+ count at Week X) - (CD4+ count at baseline). (NCT00326963)
Timeframe: Baseline (Day 1), Weeks 4, 12, and 24

Interventioncells/mm^3 (Mean)
At Week 4; n = 114At Week 12; n = 109At Week 24; n = 105
Enfuvirtide+PI+ARV's568389

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Change From Baseline in Log 10 Plasma HIV-1 RNA Viral Load

Summary statistics for change from baseline in plasma HIV-1 RNA count were presented. Change from baseline in plasma HIV-1 RNA count was derived as follows: Change from baseline = (plasma HIV-1 RNA count at Week X) - (plasma HIV-1 RNA count at baseline). (NCT00326963)
Timeframe: Baseline (Day 1), Weeks 4, 12, and 24

Interventioncopies/mL (Mean)
At Week 4; n = 116At Week 12; n = 109At Week 24; n = 107
Enfuvirtide+PI+ARV's-2.22-2.51-2.61

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Descriptive Summary of ISR Parameters (ie, Severity and Frequency of Pain and Symptoms) by Injection Device Based on an ISR Grading Tool.

Injection site reactions (ISRs) referred to any localized sign or symptom, including erythema, induration, pruritus, nodules, ecchymosis (degree of bruising/ discoloration), and pain/discomfort. Injection site reactions were monitored by trained study personnel at weeks 1, 4, 12, 16, and 24. Grades 0 through 4 are a measure of intensity, not seriousness. Thus, a grade 3 or grade 4 sign or symptom could be severe, but not necessarily serious. Only active, ongoing ISR were counted. The maximum severity grade for pain/discomfort since the last visit at any injection site was recorded whether or not the maximum severity of pain/discomfort was ongoing at the time of clinical evaluation. (NCT00326963)
Timeframe: Week 24

Interventionparticipants (Number)
Ongoing Pain/Discomfort, Grade 0; n= 110Ongoing Pain/Discomfort, Grade 1; n= 110Ongoing Pain/Discomfort, Grade 2; n= 110Ongoing Pain/Discomfort, Grade 3; n= 110Erythema, Grade 0; n= 110Erythema, Grade 1; n= 110Erythema, Grade 2; n= 110Erythema, Grade 3; n= 110Erythema, Grade 4; n= 110Erythema, Grade 3 & 4; n= 110Induration, Grade 0; n= 110Induration, Grade 1; n= 110Induration, Grade 2; n= 110Induration, Grade 3; n= 110Induration, Grade 4; n= 110Induration, Grade 3 & 4; n= 110Pruritus, Grade 0; n= 110Pruritus, Grade 1; n= 110Pruritus, Grade 2; n= 110Pruritus, Grade 3; n= 110Nodules and Cysts, Grade 0; n= 110Nodules and Cysts, Grade 1; n= 110Nodules and Cysts, Grade 2; n= 110Nodules and Cysts, Grade 3; n= 110Nodules and Cysts, Grade 4; n= 110Nodules and Cysts, Grade 3 & 4; n= 110Ecchymosis, Grade 0; n= 110Ecchymosis, Grade 1; n= 110Ecchymosis, Grade 2; n= 110Ecchymosis, Grade 3; n= 110Ecchymosis, Grade 4; n= 110Ecchymosis, Grade 3 & 4; n= 110
Enfuride+PI+ARV's732411168231251657121913821961300908380882136628

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Number of Participants Adhering to Enfuvirtide (ENF)

"Adherence to ENF treatment regimen was calculated using the participant's response to the query on the Participant Adherence Questionnaire case report form (CRF) about injections incomplete or missed in the last 4 days preceding the study visit. The percentage adherence to the ENF regimen at each study visit is given by: % Adherence = ([8 - the number of doses missed] / 8) x 100. The number and percentage of participants adhering to the ENF regimen were presented by adherence category (100%, ≥95%, ≥90% and ≥85%) at Weeks 4, 12, and 24." (NCT00326963)
Timeframe: Weeks 4, 12, and 24

Interventionparticipants (Number)
100%; At Week 4; n = 125≥95%; At Week 4; n = 125≥90%; At Week 4; n = 125≥85%; At Week 4; n = 125100%; At Week 12; n = 113≥95%; At Week 12; n = 113≥90%; At Week 12; n = 113≥85%; At Week 12; n = 113100%; At Week 24; n = 93≥95%; At Week 24; n = 93≥90%; At Week 24; n = 93≥85%; At Week 24; n = 93
Enfuvirtide+PI+ARV's10810810811998989810679797987

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Number of Participants Discontinuing Study Medication Due to Clinical Adverse Events

The total number and percentage of participants who discontinued the study medication (ENF) due to clinical adverse events (including clinically significant laboratory abnormalities and AIDS Clinical Trials Group (ACTG) grade≥3 laboratory toxicities) were noted and presented. (NCT00326963)
Timeframe: Up to Week 24

Interventionparticipants (Number)
Total participants with at least one AEUpper Gastrointestinal haemorrhageSepsisRash
Enfuvirtide+PI+ARV's3111

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Number of Participants Meeting Virologic Failure Criteria

The participant was considered as virologic failure at Week 12 clinic visit if patient achieved HIV-RNA <50 copies/mL at Week 4, and HIV-RNA > 50 copies/mL at Week 12, and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after Week 12 or if participants failed to achieve a viral load decrease from baseline greater or equal to 0.5 log10 at Week 12 and failed to achieve a viral load decrease from baseline greater or equal to 0.5 log10 confirmed at 2 to 4 weeks after Week 12. The participant was considered as virologic failure at Week 24 clinic visit if participant achieved HIV-RNA <50 copies/mL at week 12, and HIV-RNA >50 copies/mL at week 24/early discontinuation, and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after week 24/early discontinuation or HIV-RNA >50 copies/mL at any time up to week 24 and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after week 24/early discontinuation. (NCT00326963)
Timeframe: Weeks 12 and 24

Interventionparticipants (Number)
Confirmed Failure; At Week 12Confirmed Failure; At Week 24Suspected Failure; At Week 12Suspected Failure; At Week 24
Enfuvirtide+PI+ARV's2101945

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Number of Participants With Any Adverse Event (AE) and Serious Adverse Event (SAE)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAEs are defined as those events that were fatal or immediately life-threatening, and those events that resulted in hospitalization; prolonged an existing hospitalization; resulted in disability; or was a congenital anomaly. (NCT00326963)
Timeframe: Up to Week 28

Interventionparticipants (Number)
Number of participants with at least one AENumber of participants with at least one SAE
Enfuvirtide+PI+ARV's1513

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Number of Participants With HIV-1 RNA Viral Load <50 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 4 and Week 12 clinic visit. The number of participants with HIV-1 RNA results <50 copies/mL is reported. (NCT00326963)
Timeframe: Week 4 and 12

Interventionparticipants (Number)
Imputation by neighboring visit values; At Week 4Without imputation by neighboring visit; At Week 4Imputation by neighboring visit values; At Week 12Without imputation by neighboring visit;At Week 12
Enfuvirtide+PI+ARV's28286463

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Number of Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Viral Load <50 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 24 clinic visit. The number of participants with HIV-1 RNA viral load results <50 copies/mL is reported. (NCT00326963)
Timeframe: Week 24

Interventionparticipants (Number)
Imputation by neighboring visit values; At Week 24Without imputation by neighboring visit;At Week 24
Enfuvirtide+PI+ARV's7978

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Percentage of Participants Adhering to ENF

"Adherence to ENF treatment regimen was calculated using the participant's response to the query on the Participant Adherence Questionnaire case report form (CRF) about injections incomplete or missed in the last 4 days preceding the study visit. The percentage adherence to the ENF regimen at each study visit is given by: % Adherence = ([8 - the number of doses missed] / 8) x 100. The number and percentage of participants adhering to the ENF regimen were presented by adherence category (100%, ≥95%, ≥90% and ≥85%) at Weeks 4, 12, and 24." (NCT00326963)
Timeframe: Weeks 4, 12, and 24

InterventionPercentage of Participants (Number)
100%; At Week 4; n = 125≥95%; At Week 4; n = 125≥90%; At Week 4; n = 125≥85%; At Week 4; n = 125100%; At Week 12; n = 113≥95%; At Week 12; n = 113≥90%; At Week 12; n = 113≥85%; At Week 12; n = 113100%; At Week 24; n = 93≥95%; At Week 24; n = 93≥90%; At Week 24; n = 93≥85%; At Week 24; n = 93
Enfuvirtide+PI+ARV's86.486.486.495.286.786.786.793.884.984.984.993.5

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Percentage of Participants Meeting Virologic Failure Criteria

The participant was considered as virologic failure at Week 12 clinic visit if patient achieved HIV-RNA <50 copies/mL at Week 4, and HIV-RNA > 50 copies/mL at Week 12, and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after Week 12 or if participants failed to achieve a viral load decrease from baseline greater or equal to 0.5 log10 at Week 12 and failed to achieve a viral load decrease from baseline greater or equal to 0.5 log10 confirmed at 2 to 4 weeks after Week 12. The participant was considered as virologic failure at Week 24 clinic visit if participant achieved HIV-RNA <50 copies/mL at week 12, and HIV-RNA >50 copies/mL at week 24/early discontinuation, and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after week 24/early discontinuation or HIV-RNA >50 copies/mL at any time up to week 24 and HIV-RNA >50 copies/mL confirmed at 2 to 4 weeks after week 24/early discontinuation. (NCT00326963)
Timeframe: Weeks 12 and 24

InterventionPercentage of participants (Number)
Confirmed Failure; At Week 12Confirmed Failure; At Week 24Suspected Failure; At Week 12Suspected Failure; At Week 24
Enfuvirtide+PI+ARV's1.57.614.534.4

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Percentage of Participants With HIV-1 RNA Viral Load <400 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 4, Week 12, and Week 24 clinic visit. The number of participants with HIV-1 RNA Viral Load results <400 copies/mL is reported. (NCT00326963)
Timeframe: Weeks 4, 12, and 24

InterventionPercentage of participants (Number)
Imputation by neighboring visit values; At Week 4Imputation by neighboring visit values; At Week 12Imputation by neighboring visit values; At Week 24Without imputation by neighboring visit;At Week 4Without imputation by neighboring visit;At Week 12Without imputation by neighboring visit;At Week 24
Enfuvirtide+PI+ARV's56.567.972.556.567.271.8

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Percentage of Participants With HIV-1 RNA Viral Load <50 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 24 clinic visit. The percentage of participants with HIV-1 RNA results <50 copies/mL is reported. (NCT00326963)
Timeframe: Week 24

InterventionPercentage of Participants (Number)
Imputation by neighboring visit values; At Week 24Without imputation by neighboring visit;At Week 24
Enfuvirtide+PI+ARV's60.359.5

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Percentage of Participants With HIV-1 RNA Viral Load <50 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 4 and Week 12 clinic visit. The percentage of participants with HIV-1 RNA Viral Load results <50 copies/mL is reported. (NCT00326963)
Timeframe: Week 4 and 12

InterventionPercentage of Participants (Number)
Imputation by neighboring visit values; At Week 4Without imputation by neighboring visit; At Week 4Imputation by neighboring visit values; At Week 12Without imputation by neighboring visit;At Week 12
Enfuvirtide+PI+ARV's21.421.448.948.1

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Number of Participants With HIV-1 RNA Viral Load <400 Copies/mL

Blood samples for HIV-1 RNA viral load measurement were collected at the Week 4, Week 12, and Week 24 clinic visit. The number of participants with HIV-1 RNA Viral Load results <400 copies/mL is reported. (NCT00326963)
Timeframe: Weeks 4, 12, and 24

Interventionparticipants (Number)
Imputation by neighboring visit values; At Week 4Imputation by neighboring visit values; At Week 12Imputation by neighboring visit values; At Week 24Without imputation by neighboring visit;At Week 4Without imputation by neighboring visit;At Week 12Without imputation by neighboring visit;At Week 24
Enfuvirtide+PI+ARV's748995748894

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Number of Participants With 1 or More Injection Site Reactions Meeting the Criteria of an Serious Adverse Event

Injection site reactions (ISRs) referred to any localized sign or symptom, including erythema, induration, pruritus, nodules, ecchymosis (degree of bruising/ discoloration), and pain/discomfort. Injection site reactions were monitored by trained study personnel at weeks 1, 4, 12, 16, and 24. Interruption of ENF for toxicity management of recurrent local grade 3 or 4 ISRs until the sign or symptom resolved to grade 2 was at the discretion of the investigator. Any individual injection site signs or symptoms meeting the criteria for a serious adverse event (SAE) had to be reported as an SAE. In the event of a serious ISR, the participant was to immediately discontinue ENF and withdraw from the study. If the participant was not already hospitalized, serious ISRs required a clinic visit within 72 hours of the event. (NCT00326963)
Timeframe: Week 1 to Week 24

Interventionparticipants (Number)
Enfuvirtide+PI+ARV's0

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Change From Baseline to Week 24 in Cluster Differentiation Antigen Four Positive (CD4+) Cell Counts

Change from Baseline in CD4+ Cell Counts at Week 24. Least squares means were calculated from an ANCOVA model with treatment as an independent variable. (NCT00487188)
Timeframe: Baseline and Week 24

Interventioncells/mm^3 (Least Squares Mean)
ENF+HAART20.81
HAART17.88

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Number of Participants With Adverse Events (AEs) During the Induction Phase

A serious AE (SAE) is an event which: results in death, is life-threatening, disabling or incapacitating; is a congenital anomaly in the offspring of a patient who received study drug; requires or prolongs inpatient hospitalization; jeopardizes the patient or require medical or surgical intervention to prevent one of the outcomes above; any Grade 4 laboratory value considered by the investigator clinically significant or that requires an action; any injection site reaction that meets SAE criteria above. Non-serious AEs reported include pneumonia and non-serious AEs that led to discontinuation. (NCT00487188)
Timeframe: Start of the study treatment until the end of the Induction Phase (Week 12 to Week 32)

,
Interventionparticipants (Number)
Serious Adverse EventNon-serious Adverse EventAdverse Events Leading to Withdrawal
ENF+HAART335
HAART311

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Percentage of Participants Maintaining CD4+ Count During the Maintenance Phase

Maintenance of CD4+ count defined as having greater than or equal to 200 cells/mm^3 at Baseline 2 (BL2) and greater than or equal to 200 cells/mm^3 at Week 48. (NCT00487188)
Timeframe: Baseline 2 to Week 48.

,,
Interventionpercentage of participants (Number)
Week 48 CD4+ Count ≥200 cells/mm^3Week 48 CD4+ Count Missing
ENF + HAART66.6733.33
HAART75.0025.00
HAART (ENF Removed)75.0012.50

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Percentage of Participants With Improvement in CD4+ Count During the Maintenance Phase

Improvement of CD4+ count defined as having from 100 to less than 200 CD4+ cells/mm^3 at Baseline 2 (BL2) and greater than or equal to 200 cells/mm^3 at Week 48. (NCT00487188)
Timeframe: Baseline 2 to Week 48.

,
Interventionpercentage of participants (Number)
Week 48 CD4+ Count ≥200 cells/mm^3Week 48 CD4+ Count Missing
ENF + HAART100.000
HAART (ENF Removed)100.000

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Number of Participants With Viral Suppression: HIV-1 RNA < 50 Copies/mL During the Induction Phase

Participants whose viral load achieved suppression (HIV-1 RNA < 50 copies/mL) at Week 24 at the latest, confirmed at Week 28 (2 consecutive assessments ≥ 28 days apart) were defined as responders. Patients who discontinued the study or did not respond to assigned treatment by week 28 were considered as non-responders. (NCT00487188)
Timeframe: From Baseline 1 to Week 28

InterventionParticipants (Number)
ENF+HAART20
HAART8

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Number of Participants With Viral Suppression HIV-1 RNA < 400 Copies/mL During the Induction Phase

Participants whose viral load achieved suppression (HIV-1 RNA < 400 copies/mL) by Week 24 at the latest, confirmed at Week 28 (2 consecutive assessments ≥ 28 days apart) were defined as responders. Patients who discontinued the study or did not respond to assigned treatment by Week 28 were considered as non-responders. (NCT00487188)
Timeframe: From Baseline 1 to Week 28

InterventionParticipants (Number)
ENF+HAART21
HAART8

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Change From Baseline to Week 48 in Cluster Differentiation Antigen Four Positive (CD4) Cell Counts

Change from Baseline in CD4 Cell Counts at Week 48. Least squares means were calculated from an ANCOVA model with treatment and baseline CD4 count as independent variables. (NCT00487188)
Timeframe: Baseline 1 and Week 48

Interventioncells/mm^3 (Least Squares Mean)
ENF+HAART73.09
HAART50.79

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Change From Baseline to Week 24 in Viral Load

"Change from Baseline in log10 HIV-1 RNA at Week 24. Least squares means were calculated from an analysis of covariance (ANCOVA) model with treatment, a flag variable removed ENF at re-randomization and Baseline viral load as independent variables." (NCT00487188)
Timeframe: Baseline and Week 24

Interventionlog10 copies/mL (Least Squares Mean)
ENF+HAART-1.402
HAART-1.156

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Time to Virological Failure During the Maintenance Phase

"Time to virological failure (defined as HIV-1 RNA ≥ 400 copies/mL) was counted from Baseline 2 until the first of the two consecutive ≥400 copies/mL measurements.~Only patients who were qualified for entering the Maintenance Phase were included in the analyses." (NCT00487188)
Timeframe: From Baseline 2 to Week 48.

Interventiondays (Median)
ENF+HAARTNA
HAARTNA

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Time to Loss of Viral Response During the Maintenance Phase

"The time to loss of viral response (defined as HIV-1 RNA <50 copies/mL) was counted from Baseline 2 until the first of two consecutive ≥50 copies/mL measurements.~Only patients who were qualified for entering the Maintenance Phase were included in the analysis." (NCT00487188)
Timeframe: From Baseline 2 to Week 48.

Interventiondays (Median)
ENF+HAARTNA
HAARTNA

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Time to Achieving HIV-1 RNA < 50 Copies/mL During the Induction Phase

"The time to achieving HIV-1 RNA <50 copies/mL was counted from Baseline 1 until the first of the two consecutive <50 copies/mL measurements.~Patients who discontinued from the study or patients who did not have confirmed virological response by week 28 were classed as non-responders and censored at Week 24." (NCT00487188)
Timeframe: Baseline 1 until Week 28.

Interventiondays (Median)
ENF+HAART57.0
HAART141.0

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Percentage of Maintenance Phase Participants With Viral Load < 50 Copies/mL at 48 Weeks

The percentage of participants from the Maintenance Phase who maintained HIV-1 RNA < 50 copies/mL at Week 48. Patients who discontinued from the study, rebounded to ≥ 50 copies/mL (i.e., had two consecutive readings ≥ 50 copies/mL), had missing data or had virological failure by Week 48 were classed as non-responders. (NCT00487188)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ENF+HAART73.7
HAART50.0

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Percentage of Induction Phase Participants With Viral Load < 50 Copies/mL at 48 Weeks

The percentage of participants from the Induction Phase who maintained HIV-1 RNA < 50 Copies/mL at Week 48. Patients who discontinued from the study, rebounded to ≥ 50 copies/mL (i.e., had two consecutive readings ≥ 50 copies/mL), had missing data or had virological failure by Week 48 were classed as non-responders. (NCT00487188)
Timeframe: Week 48

Interventionpercentage of participants (Number)
ENF+HAART45.2
HAART25.0

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Number of Participants With Virological Failure During the Maintenance Phase

Virological failure was defined by 2 consecutive HIV-1 RNA values ≥ 400 copies/mL during the Maintenance Phase. (NCT00487188)
Timeframe: From Baseline 2 to Week 48.

InterventionParticipants (Number)
ENF+HAART3
HAART0

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Number of Patients in Phase II of the Study With HIV-1 RNA ≤ 50 Copies/mL at Week II-16

(NCT00488059)
Timeframe: Week II-16

Interventionparticipants (Number)
Phase II Arm A: Phase I Then ENF 90 mg SC BID5
Phase II Arm B: Phase I Then ENF 180mg SC QD3

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CD4+ Lymphocyte Count Change From Baseline

"Change from study Phase I baseline in CD4+ lymphocyte count at Phase II study Weeks II - 1, 12, 16, and LOCF by treatment arm.~Change from study Phase II baseline in CD4+ lymphocyte count at Phase II study weeks II - 12 and 16." (NCT00488059)
Timeframe: Phase I Baseline and Phase II Weeks II-1, 12, 16, and LOCF

,
Interventioncells/mm3 (Median)
Phase I baseline to Week 1 of Phase II (n=8,5)Phase I baseline to Week 12 of Phase II (n=7,4)Phase I baseline to Week 16 of Phase II (n=6,4)
Phase II Arm A: Phase I Then ENF 90mg BID2283.061.0
Phase II Arm B: Phase I Then ENF 180mg QD118.0174.5179.0

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HIV-1 RNA Viral Load Change From Baseline in Phase I of the Study

Change from baseline in HIV-1 RNA (log10 copies/mL) at study Weeks I-4, 8, 12 & LOCF for ITT patients in Phase I of the study (NCT00488059)
Timeframe: Baseline and Weeks 4, 8, 12 & LOCF

Interventionlog10 copies/mL (Mean)
Baseline (N=29)change at Week 4 (n=27)change at Week 8 (n=24)change at Week 12 (n=14)change at Week 16 (n=10)change at LOCF (n=27)
Phase I: ENF 90mg SC BID4.42.12.02.42.31.9

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Number of Patients in Phase I of the Study With a Confirmed HIV-1 RNA Viral Load ≤ 50 Copies/mL

Virologic responders were defined as patients who had an initial HIV-1 RNA assessment <= 50 copies/mL during Phase I at any visit between Week I-4 and Week I-12 and a confirmatory viral load assessment ≤ 50 copies/mL at the next visit (Week I-8 to Week II-16) (NCT00488059)
Timeframe: Between Week I-4 and Week I-12 of Phase I of the study

Interventionparticipants (Number)
Week 8Week 12Week 16
Phase I: ENF 90mg SC BID851

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Percentage of Patients With Ongoing Injection Site Reactions (ISRs)

(NCT00488059)
Timeframe: Phase I and II

,,
InterventionPercentage of patients (Number)
Any typePain/discomfortErythemaIndurationPruritusNodulesEcchymosis
Phase I: ENF 90mg SC BID92528080445640
Phase II - Arm A10042.971.410028.657.114.3
Phase II - Arm B10060100100208020

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Virologic Response Over Time in Phase I of the Study

The number of intent-to-treat (ITT) participants with HIV-1 RNA <= 50 copies/mL and HIV-1 RNA < 400 copies/mL by study week are summarized below. (NCT00488059)
Timeframe: Weeks 4, 8 & 12

Interventionparticipants (Number)
Week 4 (<= 50 copies/mL)Week 4 (< 400 copies/mL)Week 8 (<= 50 copies/mL)Week 8 (< 400 copies/mL)Week 12 (<= 50 copies/mL)Week 12 (< 400 copies/mL)
Phase I: ENF 90mg SC BID112214221419

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Virologic Response Over Time in Phase II of the Study

The number of intent-to-treat (ITT) participants with HIV-1 RNA <= 50 copies/mL and HIV-1 RNA < 400 copies/mL by study week. (NCT00488059)
Timeframe: Weeks II-4, 8, 12 & 16

,
Interventionparticipants (Number)
Week 4 (<= 50 copies/mL)Week 4 (< 400 copies/mL)Week 8 (<= 50 copies/mL)Week 8 (< 400 copies/mL)Week 12 (<= 50 copies/mL)Week 12 (< 400 copies/mL)Week 16 (<= 50 copies/mL)Week 16 (< 400 copies/mL)
Phase II Arm A: Phase I Then ENF 90mg SC BID56676756
Phase II Arm B: Phase I Then ENF 180mg SC QD44444434

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Change in Plasma HIV-1 Viral Load From Baseline to Week 1

Method of Kaplan and Meier used to accommodate left-censoring for those whose week 1 levels < 50 copies/mL. (NCT00537394)
Timeframe: From baseline to Week 1 evaluation

Interventionlog10 copies/mL (Median)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)1.3
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)1.4

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Number of Participants With Change in Virus Co-receptor Tropism Among Those With R5-only Tropic Virus at Study Entry

HIV Co-receptor tropism test result of either dual/mixed or evidence of X4 using virus from sample collected at confirmed virologic failure. (NCT00537394)
Timeframe: From study entry to time of confirmed virological failure (up to 96 weeks)

Interventionparticipants (Number)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)3
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)2

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Participants With Newly Acquired HIV Drug Resistance Between Study Entry and Confirmed Virologic Failure

Defined among the subgroup of participants experiencing the outcome of confirmed virologic failure. Newly acquired HIV drug resistance is defined as one or more ARVs with partial resistance or resistance when pre-entry resistance was fully sensitive or resistant when pre-entry resistance was fully sensitive or partially sensitive. The ARVs included for resistance acquisition included the following: darunavir/ritonavir; etravirine, tipranavir, tenofovir, emtracitabine, lamivudine, zidovudine, abacavir. (NCT00537394)
Timeframe: Between baseline and confirmed virologic failure (up to 96 weeks)

Interventionparticipants (Number)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)18
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)13

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Percent of Participants With Regimen Failure, Defined as a Confirmed Virologic Failure or Discontinuation of Randomized NRTI Component of Study Treatment

Virologic failure defined as confirmed plasma HIV-1 RNA meeting 1 of the following 4 criteria: < 1.0 log10 copies/mL reduction from baseline level and >= 200 copies/mL at or after week 12 evaluation; >= 200 copies/mL after 1 measurement < 200 copies/mL; absence of any values < 200 copies/mL by and including week 24 evaluation; >= 200 copies/mL at week 48 evaluation. Discontinuation of Randomized NRTI component of Study Treatment is defined as permanently stopping all NRTIs among those randomized to add NRTIs, or starting any NRTI among those randomized to omit NRTIs. Subjects leaving the study for reasons other than death, relocation, incarceration, or site closure were reviewed for the discontinuation outcome by a blinded, independent panel. Additionally, any participant failing to start study treatment after randomization and prior to closure was also reviewed. Results report percent of participants reaching regimen failure outcome by week 48 evaluation using Kaplan-Meier method. (NCT00537394)
Timeframe: From study entry to end of Week 48 evaluation window

Interventionpercentage of participants (Number)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)26.0
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)29.8

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Change in Cardiovascular Risk Score From Baseline

Cardiovascular risk score defined by Framingham providing an estimate of the probability of developing cardiovascular disease over the next 10-year period. Persons with a historical cardiovascular event (CAD, cerebro- or peripheral- vascular disorder, MI or stroke), were excluded, and scores were not calculated at follow-up times after individuals had a cardiovascular event. Missing values for input data (e.g. smoking status) resulted in a missing value for Framingham score. (NCT00537394)
Timeframe: At Weeks 24, 48, and 96

,
Interventionunits on a scale (Mean)
Week 24 (N= 150; N=147)Week 48 (N=143; N=144)Week 96 (N=129; N=132)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)-0.70.10.5
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)0.30.81.1

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Change in CD4 Count From Baseline

Baseline CD4 calculated as average of pre-entry and entry values. Closest observed result between 42 and up to 54 weeks (for week 48) or between 90 and up to 110 weeks (for week 96), used if multiple results available. Missing values excluded. (NCT00537394)
Timeframe: From study entry to Weeks 48 and 96

,
Interventioncells/mm^3 (Median)
Change from entry to week 48 (N=166; N=163)Change from entry to week 96 (N= 154; N=157)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)105.5140.8
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)89.5115.5

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Change in Fasting Non-HDL Cholesterol From Baseline

Fasting non-HDL cholesterol calculated from difference between fasting total cholesterol and fasting HDL level. Missing values and non-fasting values excluded. (NCT00537394)
Timeframe: From study entry to Weeks 24, 48

,
Interventionmg/dL (Mean)
Change from baseline to week 24 (N=131; N=121)Change from baseline to week 48 (N=125 ; N=117)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)4.17.6
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)20.819.8

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Change in Summarized Quality of Life Score

Quality-of-life score at each evaluation based upon a single question assessing participants' self-report of general health with a range of 0 (representing worst health status) to 100 (representing perfect health). (NCT00537394)
Timeframe: At study entry and Weeks 24, 48, 96

,
Interventionunits on a scale (Median)
Change from baseline to week 24 (N=165; N=165)Change from baseline to week 48 (N=161; N=158)Change from baseline to week 96 (N=155; N=154)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)000
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)500.5

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Number of Participants Self-reporting Non-adherence to Assigned Study ARVS (Excluding NRTIs, if Applicable)

Results represent self-report of non-adherence during the 4-day period prior to the outcome evaluation visit. Participants in follow-up for whom these data are missing for any reason are inferred as not-adherent. (NCT00537394)
Timeframe: At Weeks 24 and 48

,
Interventionparticipants (Number)
Week 24 (N=170; N=172)Week 48 (N=167; N=163)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)2530
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)2626

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Number of Participants With Plasma HIV-1 Viral Load < 50 Copies/ml

Number of participants with plasma HIV-1 Viral load < 50 copies/mL at study visit weeks 24, 48, and 96. Closest observed result between 20 and up to 30 weeks (for week 24), between 42 and up to 54 (for week 48), and between 90 and up to 110 (for week 96) used if multiple results available. Missing values excluded. (NCT00537394)
Timeframe: At Weeks 24, 48, 96

,
Interventionparticipants (Number)
Week 24: Number with RNA < 50 c/mL (N=170; N=171)Week 48: Number with RNA < 50 c/mL (N=169; N=165)Week 96: Number with RNA < 50 c/mL (N=158; N=158)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)122112107
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)117106109

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Time From Randomization to Confirmed Virological Failure

Virologic failure defined as confirmed (two consecutive) plasma HIV-1 RNA meeting 1 of the following 4 criteria: < 1.0 log10 copies/mL reduction from baseline level and >= 200 copies/mL at or after week 12 evaluation; >= 200 copies/mL after 1 measurement < 200 copies/mL; absence of any values < 200 copies/mL by and including week 24 evaluation; >= 200 copies/mL at week 48 evaluation. Event time was the scheduled study visit week when the initial plasma HIV-1 RNA specimen meeting the failure definition was collected. Censoring time was the latest scheduled study visit week when a plasma HIV-1 RNA specimen was collected and tested. (NCT00537394)
Timeframe: From randomization to week 96 study visit

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)121248
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)121248

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Time From Randomization to Discontinuation of Randomized NRTI Component of Study Treatment

Discontinuation of Randomized NRTI component of Study Treatment is defined as permanently stopping all NRTIs among those randomized to add NRTIs, or starting any NRTI among those randomized to omit NRTIs. Subjects leaving the study for reasons other than death, relocation, incarceration, or site closure were reviewed for meeting this outcome by a blinded, independent panel. Additionally, any participant failing to start study treatment after randomization and prior to closure was also reviewed. Event times were scheduled study weeks when discontinuation events occurred. Censoring times were latest scheduled study visit weeks with evaluation. (NCT00537394)
Timeframe: From randomization to week 96 study visit

,
Interventionweeks (Number)
1st percentile5th percentile10th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)036NA
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)03648

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Time From Treatment Dispensation to First Grade 3 or Higher (and at Least One Grade Higher Than Baseline) Signs/Symptom or Laboratory Abnormality

Events following permanent discontinuation of NRTI assignment are excluded (i.e. censoring at time of this event, if applicable). Week 96 study visit could occur up to 110 weeks following randomization. Censoring time was the latest study visit when participant was evaluated or when NRTI assignment was discontinued (when applicable). Event time was the exact number of weeks following treatment initiation when the qualifying sign/symptom started (for those safety events triggered by a sign/symptom), or exact number of weeks following treatment initiation when specimen from qualifying laboratory result was drawn (for those safety events triggered by a laboratory abnormality). (NCT00537394)
Timeframe: From treatment dispensation to week 96 study visit

,
Interventionweeks (Number)
5th percentile25th percentile50th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)3.124.7NA
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)3.925.397.7

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Time From Treatment Dispensation to First Study ARV Modification (Excluding NRTIs, if Applicable)

First study ARV modification included any discontinuation or substitution of any chosen and initiated ARV for any reason. Events prompting study medication change could include protocol required (e.g. safety), protocol recommended but not required (e.g. virologic failure), or participant motivated (such as non-adherence, loss to follow-up or death; in other words, not protocol recommended or required). Event times were the exact weeks from treatment initiation to the time of qualifying regimen modification. Censoring times were the exact weeks from treatment initiation to the last date of study drugs. The week 96 (final study visit) could occur up through 110 weeks following randomization. (NCT00537394)
Timeframe: From treatment dispensation to week 96 study visit

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)9.031.198.0
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)24.038.0NA

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Time From Treatment Dispensation to Serious Non-AIDS-defining Events

Serious Non-AIDS defining Events were adjudicated by independent and blinded review and possible events included serious diagnoses in the following disease areas: liver, cardiovascular, end-stage renal, non-AIDS malignancy, and diabetes mellitus. Week 96 study visit could take place up to 110 weeks following randomization. Event times were the exact weeks following treatment initiation corresponding to the diagnosis dates of the qualifying serious non-AIDS defining events. Censoring times were the weeks following treatment initiation corresponding to the latest study visit. (NCT00537394)
Timeframe: From treatment initiation to week 96 study visit

,
Interventionweeks (Number)
1st percentile5th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)4.960.0
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)29.3NA

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Number of Participants With Premature Withdrawal Due to Adverse Events

(NCT02582983)
Timeframe: Up to 96 weeks

Interventionparticipants (Number)
Enfuvirtide1

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Number of Participants With Serious Adverse Events (SAEs)

"A serious adverse event is any untoward medical occurrence that at any dose: results in death, or is life-threatening, or requires inpatient hospitalization or prolongation of existing hospitalization, or results in persistent or significant disability/incapacity, or is a congenital anomaly/birth defect. The term life-threatening in the definition of serious refers to an event in which the patient was at risk of death at the time of the event, not an event which hypothetically might have caused death if it were more severe." (NCT02582983)
Timeframe: Up to 28 days after permanent discontinuation of study treatment (approximately 100 weeks)

Interventionparticipants (Number)
Enfuvirtide6

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