Products
Maraviroc is commercially available in the form of film-coated tablets (Celsentri, in some countries: Selzentry). It has been approved in many countries since 2008.
Structure and properties
Maraviroc (C29H41F2N5O, Mr = 513.7 g/mol) exists as a white to pale colored powder that is soluble in water.
Effects
Maraviroc (ATC J05AX09) has indirect antiviral properties. It is a selective and slowly reversible antagonist of the interaction between human CCR5 and viral gp120, preventing membrane fusion and entry of HI viruses into cells.
Indications
In combination with other antiretroviral agents for the treatment of patients with HIV infection in whom only CCR5-tropic HIV-1 has been detected.
Dosage
According to the SmPC. The usual dose is between 150-600 mg. The drug is taken twice daily, independent of meals. Before treatment, patients must be proven to be infected exclusively by CCR5-tropic viruses with a test.
Contraindications
- Hypersensitivity
- Severe kidney disease
Full details of precautions and interactions can be found in the drug label.
Interactions
Maraviroc is metabolized by CYP3A4 and is a substrate of P-glycoprotein. When combined with CYP3A4 inhibitors or inducers, the dose must be adjusted accordingly. Drugs containing St. John’s wort, an inducer of CYP3A4, must not be used concomitantly because they reduce the effects of maraviroc.
Adverse effects
The most common possible adverse effects include nausea, diarrhea, fatigue, and headache. Other common side effects include anemia, depression, insomnia, indigestion, and skin rash. Liver-toxic side effects have been reported.
