Enfuvirtide is a linear 36-amino acid synthetic peptide that inhibits the fusion of HIV-1 with CD4 cells. Enfuvirtide works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide interferes with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes. Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. Enfuvirtide is indicated for the treatment of HIV-1 infection, in combination therapy with other antiretrovirals, in patients where all other treatments have failed. Common adverse drug reactions associated with enfuvirtide therapy include: injection site reactions (pain, hardening of skin, erythema, nodules, cysts, itch; experienced by nearly all patients, particularly in the first week), peripheral neuropathy, insomnia, depression, cough, dyspnoea, anorexia, arthralgia, infections (including bacterial pneumonia) and/or eosinophilia.
Approval Year
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | FUZEON Approved UseFUZEON is an HIV-1 fusion inhibitor indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment experienced patients with HIV-1 replication despite ongoing antiretroviral therapy. Launch Date1.0475136E12 |
PubMed
Title | Date | PubMed |
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[T-20: a fusion inhibitor]. | 2002 |
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HIV medicine after Barcelona conference: interview with Howard Grossman, M.D. Interview by John S. James. | 2002 Sep 6 |
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ConFuzeon reigns. | 2003 Apr |
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Anti-HIV-1 activity of enfuvirtide (T-20) by inhibition of bystander cell death. | 2003 Apr |
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The LLSGIV stretch of the N-terminal region of HIV-1 gp41 is critical for binding to a model peptide, T20. | 2003 Apr |
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Drug cost. States concerned about Fuzeon. | 2003 Apr 11 |
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Stopping HIV fusion with enfuvirtide: the first step to extracellular HAART. | 2003 Feb |
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David Reddy--taking HIV therapy to new frontiers. Interview by Pam Das. | 2003 Feb |
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Human immunodeficiency virus type 1 attachment, coreceptor, and fusion inhibitors are active against both direct and trans infection of primary cells. | 2003 Feb |
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Anti-HIV drug updates--three drugs on the near horizon. | 2003 Jan |
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Projecting future drug expenditures--2003. | 2003 Jan 15 |
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Synthesis of maleimide-activated carbohydrates as chemoselective tags for site-specific glycosylation of peptides and proteins. | 2003 Jan-Feb |
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First fusion inhibitor for advanced HIV. | 2003 Jul |
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Large-scale manufacture of peptide therapeutics by chemical synthesis. | 2003 Jul |
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[HIV infections: further options for combination therapy]. | 2003 Jul 11 |
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FDA notifications. FDA approves Fuzeon, the first fusion inhibitor. | 2003 Jun |
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Antiviral Research--16th Annual International Conference. Satellite symposium: clinical update on antiviral drugs. 27 April-1 May 2003, Savannah, GA, USA. | 2003 Jun |
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Gateways to clinical trials. | 2003 Jun |
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Uncommon mutations at residue positions critical for enfuvirtide (T-20) resistance in enfuvirtide-naive patients infected with subtype B and non-B HIV-1 strains. | 2003 Jun 1 |
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[First fusion inhibitor is available. No entry for HIV-1 viruses]. | 2003 Jun 19 |
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Enfuvirtide (Fuzeon) for HIV Infection. | 2003 Jun 23 |
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Treatment with a new fusion inhibitor: patient issues with enfuvirtide (T-20). 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. | 2003 Mar |
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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. | 2003 Mar |
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New classes of HIV drugs on the horizon. 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. | 2003 Mar |
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Gateways to clinical trials. March 2003. | 2003 Mar |
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FUZEON (enfuvirtide, T-20). Breaking barriers or breaking the bank? | 2003 Mar |
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Fuzeon data review. | 2003 Mar |
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Long path to approval. A look back at the road to Fuzeon. | 2003 Mar |
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Entry inhibitors SCH-C, RANTES, and T-20 block HIV type 1 replication in multiple cell types. | 2003 Mar |
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T-20: most expensive AIDS drug ever at $25,000 per year? | 2003 Mar 14 |
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A phase II clinical study of the long-term safety and antiviral activity of enfuvirtide-based antiretroviral therapy. | 2003 Mar 28 |
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Fusion inhibitor approved. | 2003 May |
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Drug profile: enfuvirtide (Fuzeon, ENF, T-20). | 2003 May |
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The optimal use of enfuvirtide. | 2003 May |
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Enfuvirtide access, administration, and patient education. | 2003 May |
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Enfuvirtide. | 2003 May |
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FDA news. Price criticized for new anti-HIV drug. | 2003 May |
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Enfuvirtide approved for defusing HIV. | 2003 May |
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US FDA approves new class of HIV therapeutics. | 2003 May |
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Enfuvirtide, a new drug for HIV infection. | 2003 May 10 |
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Primary resistance mutations to fusion inhibitors and polymorphisms in gp41 sequences of HIV-1 non-B subtypes and recombinants. | 2003 May 2 |
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Fusion inhibition--a major but costly step forward in the treatment of HIV-1. | 2003 May 29 |
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Novel therapies based on mechanisms of HIV-1 cell entry. | 2003 May 29 |
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Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. | 2003 May 29 |
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HIV infection--a new drug and new costs. | 2003 May 29 |
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Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. | 2003 May 29 |
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[HIV-1 fusion inhibitor improves treatment in HIV-1-resistant patients]. | 2003 May 9 |
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New class of medications approved for advance HIV. | 2003 May-Jun |
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Inhibiting HIV-1 entry with fusion inhibitors. | 2003 Sep |
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Virus entry as a target for anti-HIV intervention. | 2003 Sep |
Sample Use Guides
Adults: Recommended dosage of Enfuvirtide is 90 mg (1 mL) twice daily injected subcutaneously into the upper arm, anterior thigh, or abdomen.
Pediatric Patients (weighing at least 11kg): Recommended dose of 2 mg/kg twice daily up to a maximum dose of 90 mg twice daily injected
subcutaneously.
Route of Administration:
Other
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NDF-RT |
N0000175616
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NCI_THESAURUS |
C1660
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J05AX07
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EMA ASSESSMENT REPORTS |
FUZEON (AUTHORIZED: HIV INFECTIONS)
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LIVERTOX |
NBK548862
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ENFUVIRTIDE
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Enfuvirtide
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TARGET -> INHIBITOR |
Enfuvirtide binds to gp41 preventing the creation of an entry pore for the capsid of the virus, keeping it out of the cell.
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Molecular Formula | CHEMICAL |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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Biological Half-life | PHARMACOKINETIC |
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