Products
Enfuvirtide is commercially available as a powder and solvent for the preparation of a solution for injection (Fuzeon). It has been approved in many countries since 2003.
Structure and properties
Enfuvirtide (C
204
H
301
N
51
O
64
, M
r
= 4492 g/mol) is a linear synthetic peptide composed of 36 natural L-amino acids. The N-terminal end is acetylated and the C-terminal end is a carboxamide. Enfuvirtide exists as an amorphous white mass and is practically insoluble in water. It has the following sequence: CH
3
CO-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH
2
Effects
Enfuvirtide (ATC J05AX07) is antiviral. It inhibits the fusion of cell membranes of HIV-1 with CD4+ cells, thereby preventing the virus from entering the host cell. Enfuvirtide mimics a portion of the viral protein gp41, which plays a central role in fusion.
Indications
For treatment of infection with HIV-1 (combination antiretroviral therapy).
Dosage
According to the SmPC. The solution for injection is administered subcutaneously twice daily.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
No relevant drug-drug interactions are known to date.
Adverse effects
The most common possible adverse effects include local reactions at the injection site, diarrhea, nausea, and fatigue.
