Enfuvirtide (Fuzeon)

Peptide

Enfuvirtide is a 36-amino acid synthetic peptide and the first FDA-approved HIV fusion inhibitor (2003). Derived from gp41, it blocks HIV entry into CD4 cells. Phase III trials showed superior viral suppression vs background regimen alone in treatment-experienced patients. Administered as 90mg subcutaneous injection twice daily.

Quick Answer

What it is

Enfuvirtide is a 36-amino acid synthetic peptide and the first FDA-approved HIV fusion inhibitor (2003). Derived from gp41, it blocks HIV entry into CD4 cells.

Key findings

  • Grade A: Viral Load Reduction (HIV Infection)
  • Grade A: CD4 Count Improvement (HIV Infection)
  • Grade A: Treatment-Experienced Efficacy (HIV Infection)

Safety

No specific caution or interaction language was detected in the current summary/outcome notes.

⚠️ Research Notice

This peptide information is for educational and research purposes only. Peptides may not be FDA-approved for human use and may only be legally available for research purposes. Consult qualified healthcare professionals before considering any peptide compounds.

ℹ️ Quick Facts: Enfuvirtide (Fuzeon)

Quick Facts: Enfuvirtide (Fuzeon)

  • Best Evidence:Grade A
  • Conditions Studied:1
  • Research Outcomes:9
  • Grade A Findings:5
  • Grade B Findings:2
  • Key Effect:HIV Infection
A5
B2
C2
D0
1 conditions · 9 outcomes

Detailed Outcomes

A
Viral Load Reduction
Phase III: Superior virological activity vs optimized background regimen alone at 24 weeks in treatment-experienced patients.
large↓Improves
A
CD4 Count Improvement
Significant immunological improvement demonstrated in pivotal Phase III trials (TORO-1 and TORO-2).
moderate↑Improves
A
Treatment-Experienced Efficacy
Effective in patients with documented resistance to NRTIs, NNRTIs, and PIs. Valuable rescue therapy option.
large↑Improves
A
Viral Suppression Rate
Higher proportion achieving viral suppression when added to optimized background therapy in clinical trials.
moderate↑Improves
A
Time to Treatment Failure
Prolonged time to virologic failure compared to control arm in Phase III studies.
moderate↑Improves
B
Immune Function
7 human trials support this finding. Human clinical trial data available.
small↑Improves
B
Safety/Tolerability
5 human trials support this finding. Human clinical trial data available.
small↑Improves
C
Liver Protection
4 human trials support this finding. Human clinical trial data available.
small↑Improves
C
Antimicrobial Activity
3 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
small↑Improves

Research Citations (34)

Quality by Design-Guided Development of Hydrogel-Forming Microneedles for Transdermal Delivery of Enfuvirtide.
(2025)
PMID: 40063825
Transdermal delivery of enfuvirtide using dissolving microneedles integrated with novel insertion and removal indicator.
(2025)
PMID: 40532764
Isopeptide Bond Bundling Superhelix for Designing Antivirals against Enveloped Viruses with Class I Fusion Proteins: A Review.
(2023)
PMID: 37005549
Metabolic, mitochondrial, renal and hepatic safety of enfuvirtide and raltegravir antiretroviral administration: Randomized crossover clinical trial in healthy volunteers.
(2019)
PMID: 31120908
Transdermal Delivery of Enfuvirtide in a Porcine Model Using a Low-Frequency, Low-Power Ultrasound Transducer Patch.
(2019)
PMID: 30583819
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
(2010)
PMID: 19805567
Fuzeon-induced collagenophagic granuloma: a peculiar granulomatous injection site reaction to Fuzeon--a case report and review of literature.
(2010)
PMID: 19223380
Efficacy and safety of switching from enfuvirtide to raltegravir in patients with virological suppression.
(2009)
PMID: 20133273
Enfuvirtide antiviral activity despite rebound viremia and resistance mutations: fitness tampering or a case of persistent braking on entering?
(2007)
PMID: 17205468
A cohort study of enfuvirtide immunological and virological efficacy in clinical practice.
(2006)
PMID: 16927284