Approved & therapeutic
Enfuvirtide
Fuzeon, T-20
Enfuvirtide is a 36-amino-acid peptide and the first HIV fusion inhibitor, used in combination with other antiretrovirals in treatment-experienced patients with ongoing viral replication despite therapy.
Also known as: Fuzeon, T-20, pentafuside
- Status
- Enfuvirtide is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Approximately 3.8 hours.
- How it's taken
- Subcutaneous injection twice daily, requiring reconstitution
- Mechanism
- Other
How Enfuvirtide works
Enfuvirtide mimics a segment of the HR2 region of the viral gp41 protein. By binding the HR1 region it prevents the hairpin conformational change gp41 must undergo to pull the viral and cell membranes together, blocking fusion and therefore entry. Because it acts outside the cell it is unaffected by the resistance mutations that compromise reverse transcriptase and protease inhibitors.
What research has looked at
- A mechanism entirely distinct from reverse transcriptase, protease and integrase inhibitors, giving activity against multi-drug-resistant virus.
- The TORO trials established added virological suppression when combined with an optimised background regimen in heavily treatment-experienced patients.
- It remains an option in salvage therapy, though its role has narrowed considerably as newer oral agents have become available.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Injection-site reactions occur in the large majority of patients — nodules, cysts, erythema, induration and pain — and are the principal reason for discontinuation. Twice-daily subcutaneous injection is required indefinitely.
- An increased rate of bacterial pneumonia was observed in trials; the label directs monitoring for pneumonia in patients with risk factors.
- Hypersensitivity reactions including rash, fever, chills, hypotension and elevated transaminases; rechallenge after a hypersensitivity reaction is not recommended.
- Peripheral neuropathy, insomnia and decreased appetite have been reported.
- Resistance develops through mutations in the gp41 HR1 binding region.
Sources
- FDA approved-drug listing for enfuvirtide · U.S. Food & Drug Administration
- DailyMed prescribing information for enfuvirtide · NIH · DailyMed
- PubMed research on enfuvirtide HIV fusion inhibitor TORO · NIH · National Library of Medicine
- DrugBank record for enfuvirtide · DrugBank
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Enfuvirtide FAQ
What is Enfuvirtide?
Enfuvirtide is a 36-amino-acid peptide and the first HIV fusion inhibitor, used in combination with other antiretrovirals in treatment-experienced patients with ongoing viral replication despite therapy.
How does Enfuvirtide work?
Enfuvirtide mimics a segment of the HR2 region of the viral gp41 protein. By binding the HR1 region it prevents the hairpin conformational change gp41 must undergo to pull the viral and cell membranes together, blocking fusion and therefore entry. Because it acts outside the cell it is unaffected by the resistance mutations that compromise reverse transcriptase and protease inhibitors.
Is Enfuvirtide FDA approved?
Yes. Enfuvirtide is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Enfuvirtide?
Reported half-life: Approximately 3.8 hours.
How is Enfuvirtide taken?
Subcutaneous injection twice daily, requiring reconstitution.
What side effects have been reported with Enfuvirtide?
Reported in the sources: Injection-site reactions occur in the large majority of patients — nodules, cysts, erythema, induration and pain — and are the principal reason for discontinuation. Twice-daily subcutaneous injection is required indefinitely; An increased rate of bacterial pneumonia was observed in trials; the label directs monitoring for pneumonia in patients with risk factors; Hypersensitivity reactions including rash, fever, chills, hypotension and elevated transaminases; rechallenge after a hypersensitivity reaction is not recommended; Peripheral neuropathy, insomnia and decreased appetite have been reported; Resistance develops through mutations in the gp41 HR1 binding region.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.