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13.10.09

Fusion inhibitors

Enfuvirtide (T20, pentafuside, Fuzeon®) prevents the fusion of viral and cell membranes, a critical step in the infection process. After locking onto a CD4 cell, a protein in the viral membrane -gp41- must undergo a conformational change to expose a fusion peptide. Enfuvirtide, a 36-aminoacid peptide, binds to one of two heptad-repeats in gp41 and prevents this conformational change. Enfuvirtide needs to be injected SC twice per day (90 mg BD for an adult), which is a big disadvantage. Enfuvirtide is associated with increased headache, insomnia, peripheral neuropathy and depression. It is very expensive.

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