GENVOYA (Elvitegravir/Cobicistat/ Emtricitabine/Tenofovir Alafenamide)

What is this medication?

GENVOYA (Elvitegravir/Cobicistat/ Emtricitabine/Tenofovir Alafenamide)
Antiretroviral, Integrase Inhibitor (Anti-HIV); Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV); Cytochrome P-450 Inhibitor

GENVOYA, a combination of Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide is officially indicated for the treatment of HIV-1 infection.

How does this medication work? 

Elvitegravir is an HIV-1 integrase strand transfer inhibitor (INSTI). Integrase is 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 HIV1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II.

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 is a nucleoside analogue of 2’-deoxycytidine. Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine triphosphate. Emtricitabine triphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination. Emtricitabine has activity that is specific to human immunodeficiency virus (HIV-1 and HIV-2) and hepatitis B virus. Emtricitabine triphosphate is a weak inhibitor of mammalian DNA polymerases that include mitochondrial DNA polymerase γ and there was no evidence of toxicity to mitochondria in vitro and in vivo.

Tenofovir Alafenamide is a phosphonamidate prodrug of tenofovir (2’-deoxyadenosine monophosphate analogue) and differs from tenofovir disoproxil fumarate which is another prodrug of tenofovir. Tenofovir alafenamide is permeable into cells and due to increased plasma stability, and intracellular activation through hydrolysis by cathepsin A, Tenofovir Alafenamide is efficient in loading Tenofovir into peripheral blood mononuclear cells (PBMCs) (including lymphocytes and other HIV target cells) and macrophages. Intracellular tenofovir is subsequently phosphorylated to the pharmacologically active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination. Tenofovir has activity that is specific to human immunodeficiency virus (HIV-1 and HIV2). Tenofovir Alafenamide displayed antiviral activity in cell culture against all HIV-1 groups. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases that include mitochondrial DNA polymerase γ. In the in vitro study, Tenofovir Alafenamide did not significantly affect mitochondrial DNA in HepG2 cells.

How should I take this medication? 

Oral: Take 1 tablet (elvitegravir 150mg/cobicistat 150mg/emtricitabine 200mg/tenofovir alafenamide 10mg) once daily.

How to Take: Take with food. 

What should I watch for while using this medication?

Before starting GENVOYA (Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide), make sure your physician is aware of any allergies or medications you currently take, if you have chronic hepatitis B, immune reconstitution syndrome, or renal toxicity. 

What if I miss a dose?

If you miss a dose of GENVOYA (Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide) within 18 hours of the time it is usually taken, take the missed dose with food as soon as possible, and then take the next dose at the regularly scheduled time. If the dose is missed by more than 18 hours, do not take the missed dose, but resume the usual dosing schedule.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light. Keep the container tightly closed.  Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication?