Enfuvirtide
approvedAlso known as: Fuzeon, T-20
Enfuvirtide (Fuzeon, T-20) is a 36-amino acid synthetic peptide that functions as a fusion inhibitor, targeting the HIV-1 envelope glycoprotein gp41. It binds to the heptad repeat 1 (HR1) region of gp41, preventing the conformational change required for viral and host cell membrane fusion. This blocks the entry of HIV into CD4+ T cells, distinguishing it from other antiretroviral classes that act on reverse transcriptase, protease, or integrase. As the first approved fusion inhibitor, it provides a unique mechanism for salvage therapy in treatment-experienced patients. Key research findings from clinical trials (e.g., TORO 1 and 2) demonstrated that enfuvirtide, when combined with an optimized background regimen, significantly reduced viral load and increased CD4+ cell counts compared to background therapy alone. Resistance mutations (e.g., G36D, V38A) in the HR1 region can emerge, limiting its durability. Pharmacokinetic studies show a short half-life (~3.8 hours) requiring twice-daily subcutaneous injection, and local injection site reactions are common. Clinically, enfuvirtide is approved for use in heavily treatment-experienced adults and children (≥6 years) with ongoing HIV-1 replication despite multiple antiretroviral regimens. Its role has diminished with the advent of more convenient oral agents, but it remains a valuable option for multidrug-resistant HIV. For research purposes only — not medical advice.
Key data
C204H301N51O64Research & studies
Enfuvirtide approval was a milestone for virus entry inhibitor-based antivirals.; Entry inhibitors include peptide-, small-molecule-, and protein-based types.; They act outside host cells, enabling use as prophylaxis and therapeutics.; The review summarizes future trends in antiviral development.
Flow chemistry was used for ligation-based assembly of polypeptides.; A novel photodesulfurization transformation was developed for use with flow NCL.; The flow platform achieves synthesis up to 2 orders of magnitude faster than batch NCL-desulfurization methods.; Rapid synthesis of enfuvirtide (HIV entry inhibitor) and somatorelin (diagnostic agent) was demonstrated.
22 antiretroviral agents are divided into 6 classes: NRTIs, NNRTIs, PIs, entry inhibitors, CCR5 inhibitors, and integrase inhibitors.; All agents are indicated for HIV-1 treatment in combination; most are active against HIV-2 except NNRTIs, enfuvirtide, and maraviroc.; Lamivudine, emtricitabine, and tenofovir are also active against hepatitis B virus.; Knowledge of class-specific and individual drug characteristics enables tailored therapeutic regimens based on patient needs and clinical setting.
Newer drugs include second-generation NRTIs, NNRTIs, PIs, and emerging classes like fusion, CCR5, integrase, and maturation inhibitors.; Issues like tolerability, drug-drug interactions, and cross-resistance remain barriers to long-term HAART success.; Initial clinical trial data for these newer drugs show promise for treatment-naïve and treatment-experienced patients.
20 anti-HIV drugs are licensed, falling into five categories: NRTIs, NtRTIs, NNRTIs, PIs, and FIs.; Over 30 compounds are under (pre)clinical development, targeting reverse transcriptase, protease, gp120, integrase, capsid proteins, or cellular proteins like CXCR4 and CCR5.; Combination therapy is the gold standard to maximize potency, minimize toxicity, and reduce resistance risk.; Once-daily dosing is ideal to optimize patient compliance and reduce treatment costs.
Frequently asked questions
What is Enfuvirtide?
Enfuvirtide (Fuzeon, T-20) is a 36-amino acid synthetic peptide that functions as a fusion inhibitor, targeting the HIV-1 envelope glycoprotein gp41. It binds to the heptad repeat 1 (HR1) region of gp41, preventing the conformational change required for viral and host cell membrane fusion. This blocks the entry of HIV
How does Enfuvirtide work?
36-aa HIV gp41 fusion inhibitor that blocks viral entry into CD4 cells; first-in-class antiretroviral fusion inhibitor.
What is the research status of Enfuvirtide?
Enfuvirtide is currently classified as approved, with 828 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Enfuvirtide?
Enfuvirtide has a molecular weight of approximately 4492 g/mol (formula C204H301N51O64).
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