Elvitegravir

Products

Elvitegravir is commercially available as film-coated tablets in fixed combination with other antiretroviral agents and cobicistat (Stribild, successor: Genvoya). It has been approved in many countries since 2013.

Structure and properties

Elvitegravir (C23H23ClFNO5, Mr = 447.9 g/mol) is a dihydroquinolone derivative. It exists as a white to yellow powder that is poorly soluble in water.

Effects

Elvitegravir (ATC J05AX11) has antiviral properties against HIV viruses. The effects are based on inhibition of viral integrase, which is necessary for insertion of viral DNA into host DNA. This inhibits viral replication. Elvitegravir is metabolized by CYP3A (see below). The concomitantly administered CYP inhibitor and pharmacokinetic booster cobicistat inhibits the metabolism of elvitegravir.

Indications

For the treatment of HIV-1 virus infection.

Dosage

According to the professional information. Tablets are taken once daily with food.

Contraindications

For complete precautions, see the drug label.

Interactions

Elvitegravir is a substrate of CYP3A and to a lesser extent of UGT1A1. Appropriate interactions must be considered.

Adverse effects

The most common potential adverse effects of the fixed combination include nausea, diarrhea, and headache.