Enfuvirtide
- Atc Codes:J05AX07
- CAS Codes:159519-65-0
- PHARMGKB ID:159519-65-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Fuzeon; Czech Republic: Fuzeon; Denmark: Fuzeon; Estonia: Fuzeon; Finland: Fuzeon; France: Fuzeon; Germany: Fuzeon; Greece: Fuzeon; Hungary: Fuzeon; Ireland: Fuzeon; Italy: Fuzeon; Latvia: Fuzeon; Lithuania: Fuzeon; Netherlands: Fuzeon; Poland: Fuzeon; Portugal: Fuzeon; Romania: Fuzeon; Slovakia: Fuzeon; Spain: Fuzeon; Sweden: Fuzeon; UK: Fuzeon.
North America
Canada: Fuzeon; USA: Fuzeon.
Latin America
Argentina: Fuzeon; Brazil: Fuzeon.
Drug combinations
Chemistry
Enfuvirtide: C~204~H~301~N~51~O~64~. Mw: 4491.88. (1) L-Phenylalaninamide, N-acetyl-L-tyrosyl-L-threonyl-L-seryl-L-leucyl-L-isoleucyl-L-histadyl-L-seryl-L-leucyl-L-isoleucyl-L-α-glutamyl-L-α-glutamyl-L-seryl-L-glutaminyl-L-asparaginyl-L-glutaminyl-L-glutaminyl-L-α-glutamyl-L-lysyl-L-asparaginyl-L-α-glutamyl-L-glutaminyl-L-α-glutamyl-L-leucyl-L-leucyl-L-α-glutamyl-L-leucyl-L-α-aspartyl-L-lysyl-L-tryptophyl-L-alanyl-L-seryl-L-leucyl-L-tryptophyl-L-asparaginyl-L-tryptophyl-; (2) N-Acetyl-L-tyrosyl-L-threonyl-L-seryl-L-leucyl-L-isoleucyl-L-histadyl-L-seryl-L-leucyl-L-isoleucyl-L-α-glutamyl-L-α-glutamyl-L-seryl-L-glutaminyl-L-asparaginyl-L-glutaminyl-L-glutaminyl-L-α-glutamyl-L-lysyl-L-asparaginyl-L-α-glutamyl-L-glutaminyl-L-α-glutamyl-L-leucyl-L-leucyl-L-α-glutamyl-L-leucyl-L-α-aspartyl-L-lysyl-L-tryptophyl-L-alanyl-L-seryl-L-leucyl-L-tryptophyl-L-asparaginyl-L-tryptophyl-L-phenylalaninamide. CAS-159519-65-0 (2001).
Pharmacologic Category
Antiretrovirals; HIV Entry and Fusion Inhibitors. (ATC-Code: J05AX07).
Mechanism of action
Enfuvirtide, a synthetic antiretroviral agent, is a human immunodeficiency virus (HIV) fusion inhibitor. It binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein. Inhibits the fusion of HIV-1 virus with CD4 cells by blocking the conformational change in gp41 required for membrane fusion and entry into CD4 cells.
Therapeutic use
Used in conjunction with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-experienced (previously treated) adults, adolescents, and pediatric patients 6 years of age or older with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies; however, there are no adequate, well-controlled studies in pregnant women. HIV-infected mothers are discouraged from breast-feeding in order to decrease potential transmission of HIV.
Unlabeled use
Contraindications
Hypersensitivity to enfuvirtide or any component of the formulation.
Warnings and precautions
May cause hypersensitivity reactions (rash, fever, nausea, vomiting, hypotension, and elevated transaminases). Immune reconstitution syndrome may be developed. Local injection site reactions are common. Pneumonia (increased incidence during clinical trials, particularly in low CD4 cell count, high initial viral load, I.V. drug use, smoking, history of lung disease). Use with caution in coagulation disorders (e.g. hemophilia) or when receiving anticoagulants (increased risk of bleeding at injection site).