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Enfuvirtide
General information
Enfuvirtide is a 36 amino acid synthetic peptide used for managing HIV treatment-experienced patients. It is a fusion inhibitor that binds to HR 1, blocking a conformational change on gp41 required for the fusion of the lipid envelope of HIV to the cytoplasmic membrane of CD4 T lymphocytes, thus preventing viral entry [ ].
Enfuvirtide has poor oral systemic availability and is formulated as a powder for subcutaneous administration after reconstitution with sterile water. The adult dose is 90 mg bd. Absorption does not vary by site of injection (for example, thigh, arm, or abdomen) [ ].
General adverse effects and adverse reactions
In trials adverse effects have included diarrhea and nausea, eosinophilia, and depression (which was the most frequent adverse reaction that led to withdrawal) [ , ].
Adverse events were reported in a phase II trial of enfuvirtide 45 mg, 67.5 mg, and 90 mg bd combined with other antiretroviral drugs [ ]. Among 52 patients who received enfuvirtide, all but one reported at least one adverse event. However, the frequency of adverse events was similar in the 19 patients in the control arm, with the exception of injection site reactions, which were reported at least once in 36 patients. However, injection site reactions occasioned drug withdrawal in only three patients receiving enfuvirtide.
Organs and systems
Hematologic
Of 14 children who were given enfuvirtide, one had grade 3 thrombocytopenia at week 65, and stopped taking the drug [ ].
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