ENFUVIRTIDE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12457443 | https://www.ncbi.nlm.nih.gov/pubmed/30836922 | https://www.ncbi.nlm.nih.gov/pubmed/30000878 | https://www.drugbank.ca/drugs/DB00109 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021481s032lbl.pdf

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
HIV-1 infection 151 Sources: https://www.drugs.com/pro/FUZEON.html	Primary		Approved 8429	FUZEON Approved Use FUZEON 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 Date 2003

PubMed

Title	Date	PubMed
Design of a peptide inhibitor that blocks the cell fusion mediated by glycoprotein 41 of human immunodeficiency virus type 1.	2000 Nov 20	11118065
Human immunodeficiency virus type 1 entry inhibitors PRO 542 and T-20 are potently synergistic in blocking virus-cell and cell-cell fusion.	2001 Apr 1	11237840
The potential for HIV fusion inhibition.	2001 Feb	11979109
Role of human immunodeficiency virus (HIV) type 1 envelope in the anti-HIV activity of the betulinic acid derivative IC9564.	2001 Jan	11120945
AIDS. Still no vaccine, but better antiviral drugs are on the way.	2001 Jan 15	11195691
Membrane-anchored peptide inhibits human immunodeficiency virus entry.	2001 Mar	11222732
T-20 small program, CD4 < 50, will enroll November 27 at 3:00 P.M.	2001 Oct 26	11768880
Antiviral drugs with extra-cellular sites of action.	2001 Sep-Oct	11590665
[T-20: a fusion inhibitor].	2002	12703471
Five new drugs enter the homestretch.	2002 Dec	12635598
New drugs show promise in attacking HIV.	2002 Dec	12572158
Enfuvirtide.	2002 Dec	12457443
New-Fill on "hold" and open-label for T-20.	2002 Jan-Feb	12216532
The safety, plasma pharmacokinetics, and antiviral activity of subcutaneous enfuvirtide (T-20), a peptide inhibitor of gp41-mediated virus fusion, in HIV-infected adults.	2002 Jul 1	12167274
Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy.	2002 Jun	12019106
Thousands face loss of treatment in ADAP money crisis.	2002 Jun 28	12161858
Therapies. Raising the limits.	2002 Jun 28	12089423
ConFuzeon reigns.	2003 Apr	12751446
The LLSGIV stretch of the N-terminal region of HIV-1 gp41 is critical for binding to a model peptide, T20.	2003 Apr	12736375
Human immunodeficiency virus type 1 attachment, coreceptor, and fusion inhibitors are active against both direct and trans infection of primary cells.	2003 Feb	12552019
Projecting future drug expenditures--2003.	2003 Jan 15	12561658
Carbohydrate-centered maleimide cluster as a new type of templates for multivalent peptide assembling. synthesis of multivalent HIV-1 gp41 peptides.	2003 Jan 2	12467718
Synthesis of maleimide-activated carbohydrates as chemoselective tags for site-specific glycosylation of peptides and proteins.	2003 Jan-Feb	12526713
First fusion inhibitor for advanced HIV.	2003 Jul	12877130
[HIV infections: further options for combination therapy].	2003 Jul 11	12899165
FDA notifications. FDA approves Fuzeon, the first fusion inhibitor.	2003 Jun	12866478
Antiviral Research--16th Annual International Conference. Satellite symposium: clinical update on antiviral drugs. 27 April-1 May 2003, Savannah, GA, USA.	2003 Jun	12861974
Gateways to clinical trials.	2003 Jun	12851663
[First fusion inhibitor is available. No entry for HIV-1 viruses].	2003 Jun 19	12891854
Enfuvirtide (Fuzeon) for HIV Infection.	2003 Jun 23	12817195
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	12765161
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	12765159
Gateways to clinical trials. March 2003.	2003 Mar	12731460
Entry inhibitors SCH-C, RANTES, and T-20 block HIV type 1 replication in multiple cell types.	2003 Mar	12689409
Enfuvirtide.	2003 May	12755128
FDA news. Price criticized for new anti-HIV drug.	2003 May	12751460
Novel therapies based on mechanisms of HIV-1 cell entry.	2003 May 29	12773651
Inhibiting HIV-1 entry with fusion inhibitors.	2003 Sep	12871113
Virus entry as a target for anti-HIV intervention.	2003 Sep	12871111

Sample Use Guides

In Vivo Use Guide

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	Protein Created by `admin` on `Sat Dec 16 16:21:24 GMT 2023` Edited by `admin` on `Sat Dec 16 16:21:24 GMT 2023`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	19OWO1T3ZE
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ENFUVIRTIDE

Official Name

English

ENFUVIRTIDE [VANDF]

Common Name

English

DP-178

Code

English

T-20

Code

English

FUZEON

Brand Name

English

DP178

Code

English

enfuvirtide [INN]

Common Name

English

ENFUVIRTIDE [EMA EPAR]

Common Name

English

ENFUVIRTIDE [USAN]

Common Name

English

Enfuvirtide [WHO-DD]

Common Name

English

T20

Code

English

ENFUVIRTIDE [MART.]

Common Name

English

ENFUVIRTIDE [MI]

Common Name

English

ENFUVIRTIDE [ORANGE BOOK]

Common Name

English

ENFUVIRTIDE [HSDB]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175616