Enfuvirtide

• CAS Number: 159519-65-0

Enfuvirtide (trade name: Fuzeon ®) is a product manufactured by Hoffmann- La Roche drug for the treatment of HIV and its later stages. It belongs to the group of fusion inhibitors ( entry inhibitors ).

Structure

Acetyl -amide YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF

Pharmacology

Enfuvirtide inhibits fusion of HIV-1 and the host cell and thus the infection of the cell. The first steps of this merger, consist in the addition of the surface protein gp120 to the CD4 receptor and a coreceptor. This addition causes conformational changes of the protein, which gp41 is exposed and a conformational change through. Characterized reach the membrane of the target cell and the virus into contact and merge with each other, whereby the virus is able to penetrate into the cell. Enfuvirtide prevents the conformational docking on gp41 and thus the infection.

Enfuvirtide is effective against HIV-1, there is no activity against HIV-2. So far, no cross-resistance between the substance and other drugs were detected.

Pharmacokinetics

Enfuvirtide is rapidly degraded in the gastrointestinal tract and thus is not orally bioavailable. After subcutaneous injection, the substance is readily absorbed. With twice-daily dosing of 90 mg, the plasma concentrations fluctuated between about 3 and 5 ug / ml. The half-life is approximately 3.8 hours.

Side effects

Enfuvirtide is well tolerated. The most common side effects are mild local reactions at the injection site. 9.4 % of patients analgesics was required. Treatment was discontinued by 3% of patients. Interactions have been not known.