Products
Entecavir is commercially available as film-coated tablets and as an oral solution (Baraclude). It has been approved in many countries since 2006. Generic versions have been available since 2017.
Structure and properties
Entecavir (C12H15N5O3, Mr = 277.3 g/mol) is a 2′-deoxyguanosine nucleoside analog. It exists as a white powder that is sparingly soluble in water. Entecavir is a prodrug and is phosphorylated in the cell to the active metabolite entecavir triphosphate.
Effects
Entecavir (ATC J05AF10) has antiviral properties. The effects are due to inhibition of HBV polymerase (HBV reverse transcriptase) and viral replication. Entecavir is an analog of the natural substrate 2′-deoxyguanosine triphosphate.
Indications
For the treatment of chronic hepatitis B.
Dosage
According to the SmPC. The drug is taken once daily on an empty stomach, that is, at least 2 hours before or 2 hours after a meal.
Contraindications
Entecavir is contraindicated in case of hypersensitivity. For complete precautions, see the drug label.
Interactions
Entecavir does not interact with CYP450. Drug-drug interactions are possible with drugs that are eliminated by the kidney like entecavir.
Adverse effects
The most common possible adverse effects include headache, fatigue, dizziness, and nausea.