Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0019693 (HIV)
 170,526 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In March 2003, enfuvirtide was approved in the USA and the European Union for the treatment of patients with HIV infection who have experienced failure or intolerable side effects of treatment with at least one representative of each antiretroviral drug class. 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. In two large phase III studies, 90 mg of enfuvirtide administered twice daily subcutaneously in addition to a background treatment of other antiretroviral drugs, had a significant favourable effect on both the plasma viral load (decrease) and the CD4 counts (increase) compared to the background treatment alone. Disadvantages of treatment with enfuvirtide are its subcutaneous administration (98% of the patients had local adverse reactions) and the high costs involved (1500 euro per patient per month).
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PMID:[Enfuvirtide, the first representative of a new class of drugs for the treatment of HIV infection : HIV fusion inhibitors]. 1452 Jul 97

The development of highly active antiretroviral therapy has improved life expectancy and reduced progression to acquired immunodeficiency syndrome in human immunodeficiency virus (HIV)-infected patients. However, resistance to currently available classes of antiretroviral drugs has become a problem, limiting the options for patients with advanced disease who have been heavily treated. Enfuvirtide (T-20; ENF), a synthetic peptide, is the first of a new class of antiretrovirals that block entry of virus into host cells. ENF interferes with conformational changes required for membrane fusion and injection of virus into the host cell. Optimal treatment of HIV infection will likely require combinations of drugs that target novel stages of HIV type 1 entry and replication.
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PMID:Enfuvirtide (T-20): a novel human immunodeficiency virus type 1 fusion inhibitor. 1452 75

Enfuvirtide is the first in a new class of drugs called fusion inhibitors. It was recently approved in Canada for the treatment of patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy. Current evidence on safety and efficacy is limited to 48-week studies. Two phase III trials found that in treatment-experienced patients failing antiretroviral treatment, the addition of subcutanous enfuvirtide to an optimized oral background antiretroviral regimen significantly reduced viral load and increased CD4 cell counts. Potential high cost and limited supply may reduce access to this treatment.
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PMID:Enfuvirtide, a new treatment for HIV infection. 1459 20

Enfuvirtide is the first of a new class of drugs, the fusion inhibitors. It is a synthetic peptide which binds to the HIV glycoprotein 41 (gp41), blocking fusion of the viral and cellular membranes. HIV isolates with reduced susceptibility to enfuvirtide have been recovered from patients receiving enfuvirtide in combination with other antiretroviral agents. Enfuvirtide 90mg (subcutaneously, twice daily) in combination with optimised background (OB) antiretroviral therapy significantly reduced plasma HIV RNA levels compared with OB alone after treatment for 24 weeks in two randomised trials involving adults with advanced HIV infection. The antiviral efficacy of enfuvirtide was maintained through to 48 weeks. At 24 and 48 weeks, the increase from baseline in the CD4+ cell count was significantly greater for patients receiving enfuvirtide plus OB than for those receiving OB alone. Enfuvirtide 30 mg/m(2) or 60 mg/m(2) in combination with other antiretroviral agents reduced plasma HIV RNA levels and increased CD4+ cell counts in a small trial involving paediatric patients with HIV infection. Local injection-site reactions were common. Lymphadenopathy and pneumonia occurred more often in patients receiving enfuvirtide plus OB than in the control group. The incidence of most other events was similar in each group.
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PMID:Enfuvirtide. 1466 54

The FDA approved enfuvirtide (Fuzeon) in spring 2003 to use with other anti-HIV drugs in children age six and older and in adults who have used anti-HIV therapy before. Enfuvirtide is in a new class of drugs called entry inhibitors. The drug works at the start of HIV's reproduction cycle by blocking its ability to infect an immune cell. This occurs at the point when HIV fuses to the cell's outer wall in order to gain entry into it.
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PMID:Enfuvirtide (Fuzeon). 1469 66

With the number of people living with HIV infection increasing and the problems of drug resistance and long-term toxicity associated with current antiretroviral agents continuing, there is a growing need for new therapy options. Enfuvirtide is the first fusion inhibitor, a new class of drug, to be licensed for the treatment of HIV infection and is a welcome addition to the arsenal of antiretrovirals. This paper, which is the result of a multidisciplinary discussion meeting, reviews current practice in treating HIV infection, the clinical data available on enfuvirtide and discusses its introduction into clinical practice. Data available to date indicate that enfuvirtide is appropriate for use in patients who have previously taken nucleoside reverse transcriptase inhibitor (NRTI), non-NRTI and protease inhibitor containing regimens and are either intolerant of them or have experienced virological failure. Enfuvirtide should ideally be used while the patient still has other active drug options available to them to combine with enfuvirtide in an effective therapy regimen.
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PMID:Enfuvirtide (Fuzeon): the first fusion inhibitor. 1471 92

Peptides are key to modern drug discovery. This article reviews the requirements for bulk production of peptides and how it affects research and production of smaller scales. Peptides, as modern drugs, are currently produced in millions in mg-scale for research purpose, in order to better understand the function of biological systems. Some newly discovered sequences form the basis of modern drugs and are now produced in multi-tons. The most popular example is the T-20 peptide (Fuzeon), which is the first peptide produced at such scale by a combination of solid phase and solution phase methodologies. This particular peptide sequence has the ability to dock on the surface of the HIV virus and block the virus from entering into a human blood cell, helping patient life conditions. A multi-ton scale production was made necessary based on the high number of patients, the socio-economical importance of the disease and the strong support by governmental institutions such as the FDA. Fuzeon is the first peptide-based drug that is produced in multi-tons on solid support. This had revolutionary effects on the whole peptide synthesis techniques in general including the production of the starting materials. It also had a positive impact on the cost-effectiveness of peptides for research, as the standard technique for producing peptides in research quantities is solid phase chemistry. The decrease of the cost of all starting materials will lead to an increase of the number of produced peptides, which will certainly bring new interesting and effective sequences to be used as novel drugs.
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PMID:From production of peptides in milligram amounts for research to multi-tons quantities for drugs of the future. 1496 8

Entry-inhibitors represent a new option in antiretroviral therapy. They prevent infection of HIV target-cells. According to their mechanism of action they can be divided into three groups: attachment-inhibitors, corezeptor-antagonists and fusion-inhibitors. The fusion-inhibitor T-20 (Enfuvirtide) will be the first substance to be licensed in 2003. It has been shown that entry-inhibition is a realistic goal for clinical use. Until now T-20 was mainly added to an optimized background regimen in intensively pretreated patients. To achieve the best efficacy a combination of substances with only slight preexisting resistance seems to be favorable. Further efforts in providing orally applicable drugs with little potential for developing resistance and with synergistic effects are required.
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PMID:[Entry inhibitors. Ring-free for a new principle of action]. 1501 78

Highly active antiretroviral therapy (HAART) based on combinations of drugs that target key enzymes in the life-cycle of human immunodeficiency virus (HIV) has considerably reduced morbidity and mortality from HIV infection since its introduction in the mid-1990s. However, the growing problem of the emergence of HIV strains that are resistant not only to individual drugs, but to whole drug classes, means that agents with new mechanisms of action are needed. Here, we describe the discovery and development of enfuvirtide (Fuzeon), the first drug to inhibit the entry of HIV-1 into host cells.
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PMID:Enfuvirtide: the first therapy to inhibit the entry of HIV-1 into host CD4 lymphocytes. 1503 35

Enfuvirtide (Fuzeon, T-20), jointly developed by Trimeris Inc. and Roche Pharmaceuticals, is the first of a new class of antiretroviral agents called fusion inhibitors that block HIV-1 entry into the host cell by binding to the gp41 subunit of the HIV-1 envelope glycoprotein. In vitro and in vivo studies have demonstrated potent antiretroviral activity among HIV-positive patients, including those with multi-drug resistant virus. The pharmacokinetic profile of subcutaneously administered enfuvirtide allows for twice-daily administration, although the possibility of once-daily dosing has not been excluded. Phase II and III clinical studies conducted to date have confirmed that enfuvirtide is an effective and safe drug for treating both adult and pediatric HIV-1-positive patients, with only mild or moderate adverse effects being reported.
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PMID:Enfuvirtide. 1514 34


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