Enfuvirtide (Fuzeon)
Overview
A 36-amino acid synthetic peptide that inhibits HIV-1 entry into CD4+ T-cells by blocking the gp41-mediated membrane fusion step. Enfuvirtide binds to the first heptad repeat (HR1) region of gp41, preventing the conformational change required for viral-cell membrane fusion. It is the first and only FDA-approved fusion inhibitor and is active against HIV-1 strains resistant to other antiretroviral drug classes.
Key Research Findings
FDA-approved in 2003 for treatment-experienced HIV-1 patients. TORO trials demonstrated approximately 1 log10 greater viral load reduction when added to optimized background regimen vs. background alone. Limited by twice-daily subcutaneous injections and frequent injection site reactions. Reserved for heavily treatment-experienced patients due to convenience limitations.
Subcutaneous injection (twice daily)
FDA Approved
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