Entecavir

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.