Sequence Information

    • DRAMP ID

    • DRAMP18181

    • Name

    • DP178 (T20, Enfuvirtide & Fuzeon)

    • Sequence

    • YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF

    • Description

    • Enfuvirtide is a 36 amino acid biomimetic peptide that is structurally similar to the HIV proteins that are responsible for the fusion of the virus to cell membranes and subsequent intracellular uptake. The first agent in the novel class of antiretroviral drugs called HIV fusion inhibitors, enfuvirtide works by inhibiting HIV-1 fusion with CD4 cells.

    • Activity

    • Anti-HIV

    • Target Organism

      • EC50=15±3.9 nM against laboratory HIV-1 NL4-3 strain (wild-type).Higher concentrations of enfuvirtide were needed to block infection with cell-free virus, with EC50s ranging from 20 nM(HIV-1LAI in CEM cells) to 240 nM(HIV-1LAI in peripheral blood mononuclear cells).

    • Reference

      • Design of a Novel HIV-1 Fusion Inhibitor That Displays a Minimal Interface for Binding Affinity(PMID: 18197613)
      • HIV fusion and its inhibition in antiretroviral therapy(PMID: 15334539)

Clinical Information

    • Medical use

    • Human Immunodeficiency Virus (HIV) Infections; AIDS

    • Company

    • Trimeris

    • Stage of Development

    • Proved by FDA

    • Comments

    • High dosage (90 mg);twice-daily administration

    • Clinical Trials

    • NCT02582983
    • NCT02569502
    • NCT00487188