Etravirine

Products

Etravirine is commercially available in tablet form (Intelence). It has been approved in many countries since 2008.

Structure and properties

Etravirine (C20H15BrN6O, Mr = 435.3 g/mol) is a brominated aminopyrimidine and a benzonitrile derivative. It exists as a white to slightly yellow-brown powder and is practically insoluble in water. Etravirine has a non-nucleoside structure and is therefore called an NNRTI (non-nucleoside reverse transcriptase inhibitor).

Effects

Etravirine (ATC J05AG) has antiviral properties against HIV-1, with effects based on inhibition of the viral enzyme reverse transcriptase, which plays a central role in viral replication. Etravirine is effective even in the presence of some resistance and has a long half-life of up to 40 hours.

Indications

In combination with other antiretroviral drugs to treat infections with HIV-1.

Dosage

According to the SmPC. Tablets are taken twice daily after meals.

Contraindications

Etravirine is contraindicated in case of hypersensitivity. Full precautions can be found in the drug label.

Interactions

Etravirine is metabolized by CYP3A, CYP2C9, and CYP2C19 and is a weak inducer of CYP3A and a weak inhibitor of CYP2C9 and CYP2C19. Corresponding drug-drug interactions are possible.

Adverse effects

The most common potential adverse effects include rash, diarrhea, hypertriglyceridemia, and nausea.