User:Ispravky/sandbox
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| Clinical data | |
|---|---|
| Trade names | Stribild (fixed-dose combination) |
| Routes of administration | oral |
| ATC code | |
| Pharmacokinetic data | |
| Protein binding | 98% |
| Metabolism | liver, via CYP3A |
| Elimination half-life | 12.9 hours |
| Excretion | liver 93%, renal 7% |
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| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEBI | |
| ChEMBL | |
| NIAID ChemDB | |
| Chemical and physical data | |
| Formula | C23H23ClFNO5 |
| Molar mass | 447.883 g/mol g·mol−1 |
| 3D model (JSmol) | |
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Elvitegravir (EVG, formerly GS-9137) is a drug used for the treatment of HIV infection. It acts as an integrase inhibitor. It was developed[1] by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008.[2][3][4] 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.[5] On September 24, 2014 the FDA approved Elvitegravir (tradename Vitekta) as a single pill formulation.[6]
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.[7]
Medical uses[edit]
In the United States, elvitegravir can be obtained either as part of the combination pill Stribild or as the single pill formulation Vitekta. [8]
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).[9]
Adverse effects[edit]
According to the package insert, the most common side effect of taking Vitekta is diarrhea. [9]
References[edit]
- ^ 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): 764–774. doi:10.1128/JVI.01534-07. PMC 2224569. PMID 17977962.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ 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. S2CID 24183976.
{{cite journal}}: CS1 maint: numeric names: authors list (link) - ^ "FDA Approval Bulletin" Accessed November 1, 2014
- ^ 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
- ^ a b "Vitekta Package Insert" Foster City, CA: Gilead Sciences, Inc.; 2014. Accessed November 1, 2014
Category:Integrase inhibitors Category:Quinolines Category:Organochlorides Category:Organofluorides Category:Japan Tobacco
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