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enfuvirtide + raltegravir + optimized background antiretroviral agents

Development stage
Unknown
Lead developer
Merck
Modality
Peptides, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Subcutaneous (enfuvirtide), Oral (raltegravir, Background ARVs)
01

Overview

This drug regimen is a **combination therapy** consisting of **enfuvirtide**, **raltegravir**, and a selection of additional antiretroviral agents tailored to the patient's resistance profile (optimized background antiretrovirals). - **Enfuvirtide** is a fusion inhibitor that blocks the HIV-1 virus from entering host cells by interfering with the conformational changes of the viral envelope glycoprotein gp41 required for membrane fusion. - **Raltegravir** is an integrase strand transfer inhibitor (INSTI); it inhibits HIV-1 integrase, preventing the integration of viral DNA into the human genome, an essential step for viral replication. - **Optimized background antiretroviral agents** are selected based on individual resistance patterns and may comprise NRTIs, PIs, NNRTIs, or other classes of HIV therapeutics. This regimen is used for **HIV-1 infection** in heavily treatment-experienced patients with multiclass resistance, often as salvage therapy to achieve or maintain viral suppression. The optimized background ARVs ensure at least one other active agent in addition to enfuvirtide and raltegravir, improving efficacy and resistance management[1][2].

Brand names
Fuzeon + Isentress + optimized background antiretroviral agents
Other names
enfuvirtide + raltegravir + optimized background ARV
02

Targets

Human immunodeficiency virus type 1 reverse transcriptasegp41 (Human immunodeficiency virus type 1 glycoprotein 41)PR (Progesterone receptor)Integrase allosteric pocket (HIV)

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