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Elvitegravir

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Elvitegravir

Elvitegravir
Systematic (IUPAC) name
6-[(3-Chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
Clinical data
Trade names Stribild (fixed-dose combination)
Pregnancy cat.
Legal status
?
Routes oral
Pharmacokinetic data
Protein binding 98%
Metabolism liver, via CYP3A
Half-life 12.9 hours
Excretion liver 93%, renal 7%
Identifiers
CAS number  YesY
ATC code J05
PubChem
ChemSpider  YesY
UNII  YesY
ChEBI  N
ChEMBL  YesY
NIAID ChemDB
Chemical data
Formula C23H23ClFNO5 
Mol. mass 447.883 g/mol
 N   

Elvitegravir (EVG, formerly GS-9137) is an integrase inhibitor used to treat HIV infection. 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

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

According to the package insert, the most common side effect of taking Vitekta is diarrhea.[9]


References

  1. ^ Gilead Press Release Phase III Clinical Trial of Elvitegravir July 22, 2008
  2. ^ Gilead Press Release Gilead and Japan Tobacco Sign Licensing Agreement for Novel HIV Integrase Inhibitor March 22, 2008
  3. ^ 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.  
  4. ^ Stellbrink HJ (2007). "Antiviral drugs in the treatment of AIDS: what is in the pipeline ?". Eur. J. Med. Res. 12 (9): 483–95.  
  5. ^ 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.  
  6. ^ "FDA Approval Bulletin" Accessed November 1, 2014
  7. ^ 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.
  8. ^ "FDA Approved Drug Listing" Accessed November 1, 2014
  9. ^ a b "Vitekta Package Insert" Foster City, CA: Gilead Sciences, Inc.; 2014. Accessed November 1, 2014


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