Products
Fostemsavir was approved in the United States in 2020 in sustained-release (ER) tablet form (Rukobia). Fostemsavir is the first agent in this drug class.
Structure and properties
Fostemsavir (C25H26N7O8P, Mr = 583.5 g/mol) is a prodrug. It is present in the drug as fostemsavirtromethamine, which is biotransformed in the body to the active metabolite temsavir.
Effects
Temsavir has antiviral properties. The effects are due to binding to the gp120 surface protein of HIV. This inhibits interaction with host cell CD4 receptors. The virus cannot dock to the cell and viral replication is inhibited.
Indications
In combination with other antiretroviral drugs for the treatment of infection with HIV-1.
Dosage
According to the SmPC. Tablets are taken twice daily (in the morning and evening), regardless of meals.
Contraindications
- Hypersensitivity
- Combination with CYP3A inducers
Full precautions can be found in the drug label.
Interactions
The active metabolite temsavir is a substrate of CYP3A, esterases, P-glycoprotein, and BCRP.
Adverse effects
Nausea occurs as the most common potential adverse effect.
