|Systematic (IUPAC) name|
|Trade names||Stribild (fixed-dose combination)|
|Metabolism||liver, via CYP3A|
|Biological half-life||12.9 hours|
|Excretion||liver 93%, renal 7%|
|Molar mass||447.883 g/mol|
|(what is this?)|
Elvitegravir (EVG, formerly GS-9137) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug Administration on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild. On September 24, 2014 the FDA approved Elvitegravir (tradename Vitekta) as a single pill formulation. On November 5, 2015 the FDA approved the drug for use in patients affected with HIV-1 as a part of a second fixed dose combination pill known as Genvoya.
According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor.
Vitekta is FDA approved to be used for the treatment of HIV-1 infection in adults who have previous treatment experience with antiretroviral therapy. It must be used in combination with a protease inhibitor that is coadministered with ritonavir as well as additional antiretroviral drug(s).
According to the package insert, the most common side effect of taking elvitegravir is diarrhea.
- Gilead Press Release Phase III Clinical Trial of Elvitegravir July 22, 2008
- Gilead Press Release Gilead and Japan Tobacco Sign Licensing Agreement for Novel HIV Integrase Inhibitor March 22, 2008
- Shimura K, Kodama E, Sakagami Y; et al. (2007). "Broad Anti-Retroviral Activity and Resistance Profile of a Novel Human Immunodeficiency Virus Integrase Inhibitor, Elvitegravir (JTK-303/GS-9137)". J Virol 82 (2): 764–74. doi:10.1128/JVI.01534-07. PMC 2224569. PMID 17977962.
- Stellbrink HJ (2007). "Antiviral drugs in the treatment of AIDS: what is in the pipeline ?". Eur. J. Med. Res. 12 (9): 483–95. PMID 17933730.
- Sax, P. E.; Dejesus, E.; Mills, A.; Zolopa, A.; Cohen, C.; Wohl, D.; Gallant, J. E.; Liu, H. C.; Zhong, L.; Yale, K.; White, K.; Kearney, B. P.; Szwarcberg, J.; Quirk, E.; Cheng, A. K.; Gs-Us-236-0102 Study, T. (2012). "Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: A randomised, double-blind, phase 3 trial, analysis of results after 48 weeks". The Lancet 379 (9835): 2439–2448. doi:10.1016/S0140-6736(12)60917-9. PMID 22748591.
- "FDA Approval Bulletin" Accessed November 1, 2014
- "Press Announcements - FDA approves new treatment for HIV". www.fda.gov. Retrieved 2016-01-10.
- Thaczuk, Derek and Carter, Michael. ICAAC: Best response to elvitegravir seen when used with T-20 and other active agents Aidsmap.com. 19 Sept. 2007.
- "FDA Approved Drug Listing" Accessed November 1, 2014
- "Vitekta Package Insert" Foster City, CA: Gilead Sciences, Inc.; 2014. Accessed November 1, 2014