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enfuvirtide

Trade name: fuzeon

PeptideapprovedFast Track FDA

Approved

Mar 13, 2003

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. — NCATS

Clinical trial activity

38 trials · 27 clinical orgs · 1 marketing orgs

Phase 1
7
Phase 2
15
Phase 3
6
Phase 4
14

Earliest trial started May 1, 1999 (NCT00002239)

Timeline

1990s

  1. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1999

    Roche — Earliest Phase 2 Sponsor(trial)

2000s

  1. Jan 1, 2001

    Roche — Earliest Phase 3 Sponsor(trial)

  2. Mar 13, 2003

    Roche — Earliest FDA Approval

  3. Mar 13, 2003

    Roche — NDA Organization

  4. Mar 13, 2003

    Roche — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedFast trackMar 13, 2003

Chemistry & pharmacology

Loading structure…

SMILES

CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Mol. weight
4491.94 g/mol
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only
Multi-specific
No

Oral

No

Parenteral

Yes

Topical

No

First in class

Sources

Also known as

  • dp178
  • dp178
  • dp178
  • dp 178
  • dp-178
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • enfuvirtide
  • envelope polyprotein gp160 precursor [contains: exterior membrane glycoprotein,gp120, transmembrane glycoprotein,gp41]
  • fuzeon
  • fuzeon
  • fuzeon
  • fuzeon
  • fuzeon
  • fuzeon
  • fuzeon t-20
  • fuzeon t-20
  • pentafuside
  • pentafuside
  • pentafuside
  • pentafuside
  • peptide t20
  • t20
  • t20
  • t-20 cpd
  • t20 peptide

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05349968Phase 1May 6, 2022Beijing Medical University, Chinese Academy of Medical Sciences, Shanxi Kangbao Pharmaceutical company
NCT04592315Phase 1Dec 10, 2020Beijing Medical University, Chinese Academy of Medical Sciences, Shanxi Kangbao Pharmaceutical company
NCT01836068Early Phase 1 (Phase 1)Jul 1, 2013Johns Hopkins University
NCT00615134Phase 2Jan 1, 2008Roche
NCT00537394Phase 3Jan 1, 2008AIDS Clinical Trials Group, Brown University, National Institute of Allergy and Infectious Diseases (NIAID), University of California, San Diego
NCT00488059Phase 4Jun 1, 2007Roche, Trimeris
NCT00461266Phase 4Apr 1, 2007Roche
NCT00337701Phase 4Jun 1, 2006Roche, Trimeris
NCT00312546Phase 1Jun 1, 2006University of North Carolina at Chapel Hill
NCT00302822Phase 3Apr 1, 2006French National Agency for Research on AIDS and Viral Hepatitis, Gilead Sciences, Roche, University of Paris
NCT00326963Phase 4Mar 1, 2006Roche, Trimeris
NCT00334022N/AFeb 1, 2006Canadian Immunodeficiency Research Collaborative, Roche, University of Toronto
NCT00487188Phase 4Nov 1, 2005Roche
NCT00657761Phase 4Sep 1, 2005Roche, University of Barcelona
NCT00233883Phase 4Aug 1, 2005Roche, Trimeris
NCT00128830Phase 2Jun 1, 2005Tibotec
NCT00120367Phase 2Apr 1, 2005Assistance Publique - Hôpitaux de Paris, French National Agency for Research on AIDS and Viral Hepatitis, Gilead Sciences, Roche
NCT02569502Phase 4Apr 1, 2005Roche
NCT00344760Phase 4Jan 1, 2005University of Maryland
NCT02733419Phase 3Dec 1, 2004Roche
Showing 20 of 38 trials
Page 1 / 2

Organizations

Research & Development (27)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
RocheFor profit221751999
TrimerisFor profit11241999
National Institute of Allergy and Infectious Diseases (NIAID)Government7741999
AIDS Clinical Trials GroupAcademic/Hospital2022003
Beijing Medical UniversityAcademic/Hospital2012020
Chinese Academy of Medical SciencesAcademic/Hospital2012020
French National Agency for Research on AIDS and Viral HepatitisGovernment2222005
Gilead SciencesFor profit2022005
Shanxi Kangbao Pharmaceutical companyFor profit2212020
University of California, San FranciscoAcademic/Hospital2122000
University of North Carolina at Chapel HillAcademic/Hospital2122003
Assistance Publique - Hôpitaux de ParisAcademic/Hospital1012005
Brown UniversityAcademic/Hospital1012008
Canadian Immunodeficiency Research CollaborativeAcademic/Hospital1112006
Columbia UniversityAcademic/Hospital1012002
Harvard UniversityAcademic/Hospital1012002
Johns Hopkins UniversityAcademic/Hospital1112013
National Heart, Lung, and Blood Institute (NHLBI)Government1012003
National Institutes of Health (NIH)Government1011999
The National Centre in HIV Epidemiology and Clinical Research, SydneyAcademic/Hospital1012003
27 organizations
Page 1 / 2

Marketing (2)

OrganizationOrg typeRelationshipDate
RocheFor profitNDAMar 13, 2003
RocheFor profitMKTGMar 13, 2003