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 |
|---|---|---|---|---|
| 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 Date2003 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Inhibiting HIV-1 entry with fusion inhibitors. | 2003-09 |
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| Virus entry as a target for anti-HIV intervention. | 2003-09 |
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| [HIV infections: further options for combination therapy]. | 2003-07-11 |
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| First fusion inhibitor for advanced HIV. | 2003-07 |
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| Large-scale manufacture of peptide therapeutics by chemical synthesis. | 2003-07 |
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| Enfuvirtide (Fuzeon) for HIV Infection. | 2003-06-23 |
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| [First fusion inhibitor is available. No entry for HIV-1 viruses]. | 2003-06-19 |
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| New class of medications approved for advance HIV. | 2003-06-10 |
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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. | 2003-06-01 |
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| FDA notifications. FDA approves Fuzeon, the first fusion inhibitor. | 2003-06 |
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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. | 2003-06 |
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| Gateways to clinical trials. | 2003-06 |
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| Fusion inhibition--a major but costly step forward in the treatment of HIV-1. | 2003-05-29 |
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| Novel therapies based on mechanisms of HIV-1 cell entry. | 2003-05-29 |
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| Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. | 2003-05-29 |
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| HIV infection--a new drug and new costs. | 2003-05-29 |
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| Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. | 2003-05-29 |
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| Enfuvirtide, a new drug for HIV infection. | 2003-05-10 |
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| [HIV-1 fusion inhibitor improves treatment in HIV-1-resistant patients]. | 2003-05-09 |
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| Primary resistance mutations to fusion inhibitors and polymorphisms in gp41 sequences of HIV-1 non-B subtypes and recombinants. | 2003-05-02 |
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| Fusion inhibitor approved. | 2003-05 |
|
| Drug profile: enfuvirtide (Fuzeon, ENF, T-20). | 2003-05 |
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| The optimal use of enfuvirtide. | 2003-05 |
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| Enfuvirtide access, administration, and patient education. | 2003-05 |
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| Enfuvirtide. | 2003-05 |
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| FDA news. Price criticized for new anti-HIV drug. | 2003-05 |
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| Enfuvirtide approved for defusing HIV. | 2003-05 |
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| US FDA approves new class of HIV therapeutics. | 2003-05 |
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| Drug cost. States concerned about Fuzeon. | 2003-04-11 |
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| ConFuzeon reigns. | 2003-04 |
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| Anti-HIV-1 activity of enfuvirtide (T-20) by inhibition of bystander cell death. | 2003-04 |
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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. | 2003-04 |
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| A phase II clinical study of the long-term safety and antiviral activity of enfuvirtide-based antiretroviral therapy. | 2003-03-28 |
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| T-20: most expensive AIDS drug ever at $25,000 per year? | 2003-03-14 |
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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. | 2003-03 |
|
| 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. | 2003-03 |
|
| 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. | 2003-03 |
|
| Gateways to clinical trials. March 2003. | 2003-03 |
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| FUZEON (enfuvirtide, T-20). Breaking barriers or breaking the bank? | 2003-03 |
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| Fuzeon data review. | 2003-03 |
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| Long path to approval. A look back at the road to Fuzeon. | 2003-03 |
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| Entry inhibitors SCH-C, RANTES, and T-20 block HIV type 1 replication in multiple cell types. | 2003-03 |
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| New antiretroviral drugs. | 2003-03 |
|
| Stopping HIV fusion with enfuvirtide: the first step to extracellular HAART. | 2003-02 |
|
| Projecting future drug expenditures--2003. | 2003-01-15 |
|
| Anti-HIV drug updates--three drugs on the near horizon. | 2003-01 |
|
| Five new drugs enter the homestretch. | 2002-12 |
|
| New drugs show promise in attacking HIV. | 2002-12 |
|
| HIV medicine after Barcelona conference: interview with Howard Grossman, M.D. Interview by John S. James. | 2002-09-06 |
|
| [T-20: a fusion inhibitor]. | 2002 |
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
| Substance Class |
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C1660
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EMA ASSESSMENT REPORTS |
FUZEON (AUTHORIZED: HIV INFECTIONS)
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NBK548862
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| Related Record | Type | Details | ||
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TARGET ORGANISM->INHIBITOR |
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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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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO_ACID_SUBSTITUTION | [1_36] | C-TERMINUS | PHENYLALANYLAMIDE | PV9T9B2S11 | ||
| AMINO_ACID_SUBSTITUTION | [1_1] | N-TERMINUS | ACETYL L-TYROSINE | DA8G610ZO5 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| 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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