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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Enfuvirtide
Jacob P Lalezari1, Andrew D Luber
1Quest Clinical Research, and University of California at San Francisco, Mount Zion Hospital, San Francisco, California, USA. drjay@questclinical.com
Abstract:
Enfuvirtide (Fuzeon, T-20), jointly developed by Trimeris Inc. and Roche Pharmaceuticals, is the first of a new class of antiretroviral agents called fusion inhibitors that block HIV-1 entry into the host cell by binding to the gp41 subunit of the HIV-1 envelope glycoprotein. In vitro and in vivo studies have demonstrated potent antiretroviral activity among HIV-positive patients, including those with multi-drug resistant virus. The pharmacokinetic profile of subcutaneously administered enfuvirtide allows for twice-daily administration, although the possibility of once-daily dosing has not been excluded. Phase II and III clinical studies conducted to date have confirmed that enfuvirtide is an effective and safe drug for treating both adult and pediatric HIV-1-positive patients, with only mild or moderate adverse effects being reported.
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