ELVITEGRAVIR

Other

Brand names: Genvoya

Oral

Mechanism of Action

12.1 Mechanism of Action GENVOYA is a fixed-dose combination of antiretroviral drugs elvitegravir (plus the CYP3A inhibitor cobicistat), emtricitabine, and tenofovir alafenamide [see Microbiology (12.4) ] . Mechanism of Action Elvitegravir: Elvitegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II. Cobicistat: Cobicistat is a selective, mechanism-based inhibitor of cytochromes P450 of the CYP3A subfamily. Inhibition of CYP3A-mediated metabolism by cobicistat enhances the systemic exposure of CYP3A substrates, such as elvitegravir, where bioavailability is limited and half-life is shortened by CYP3A-dependent metabolism. Emtricitabine: Emtric

Indications

an HIV-1 integrase strand transfer inhibitor (INSTI)

cobicistat (COBI)

a CYP3A inhibitor

and emtricitabine (FTC) and tenofovir alafenamide (TAF)

both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs)

Contraindications

• phenobarbital
• phenytoin Antimycobacterial: rifampin Antipsychotics: lurasidone
• pimozide Ergot Derivatives: dihydroergotamine
• ergotamine
• methylergonovine Herbal Products: St. John's wort ( Hypericum perforatum ) Lipid-modifying Agents: lomitapide

FDA Warnings

5 WARNINGS AND PRECAUTIONS Risk of adverse reactions or loss of virologic response due to drug interactions: The concomitant use of GENVOYA and other drugs may result in known or potentially significant drug interactions, some of which may lead to loss of therapeutic effect of GENVOYA and possible development of resistance; clinically significant adverse reactions from greater exposures of concomitant drugs; or loss of therapeutic effect of concomitant drugs
2 Risk of Adverse Reactions or Loss of Virologic Response Due to Drug Interactions The concomitant use of GENVOYA and other drugs may result in known or potentially significant drug interactions, some of which may lead to [see Contraindications (4) and Drug Interactions (7
Clinically significant adverse reactions, potentially leading to severe, life-threatening, or fatal events, from greater exposures of concomitant drugs metabolized by CYP3A
Patients taking tenofovir prodrugs who have impaired renal function and those taking nephrotoxic agents including non-steroidal anti-inflammatory drugs are at increased risk of developing renal-related adverse reactions

Known Side Effects

1 documented side effects by frequency

Anxiety

0.1-1%

Community Discussions

No community discussions found for ELVITEGRAVIR yet.

Compare With

0 available comparisons

No comparisons yet.

Formulations

Dosage Forms

Tablet

Route

Oral