Elvitegravir

Elvitegravir is an antiretroviral medication used to treat human immunodeficiency virus type 1 (HIV-1) infection. It belongs to the integrase strand transfer inhibitor (INSTI) class, which blocks the enzyme integrase that inserts viral DNA into the host cell genome, a critical step in HIV replication.

Elvitegravir is most commonly used as part of fixed-dose, once-daily regimens that include a boosting agent and a nucleoside reverse transcriptase inhibitor backbone. Notable combinations are Stribild, which contains elvitegravir with cobicistat, emtricitabine, and tenofovir disoproxil fumarate, and Genvoya, which contains elvitegravir with cobicistat, emtricitabine, and tenofovir alafenamide. These regimens are taken with food.

Pharmacologically, elvitegravir exposure is increased by cobicistat, a metabolic booster that inhibits CYP3A4. The drug is metabolized in the liver and eliminated mainly in the feces, with some renal excretion. Because of the boosting, drug interactions with other CYP3A4 inhibitors or inducers are important considerations in management.

Common adverse effects include nausea, diarrhea, headache, and fatigue. The cobicistat component can cause small, nonspecific increases in serum creatinine that do not necessarily reflect a true decrease in kidney function. Rare but serious adverse events can include liver-related toxicity and hypersensitivity reactions.

Resistance can arise through mutations in the HIV integrase gene. Monitoring of HIV-1 RNA levels and CD4 counts, along with assessment of renal and hepatic function and potential drug interactions, is recommended during therapy. Data on use in pregnancy are limited; treatment decisions should weigh potential benefits and risks.