Elvitegravir

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Elvitegravir
Elvitegravir structure.svg
Elvitegravir3D.PNG
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. B (US)
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 697761-98-1 YesY
ATC code J05AX11
PubChem CID 5277135
ChemSpider 4441060 YesY
UNII 4GDQ854U53 YesY
ChEBI CHEBI:72289 N
ChEMBL CHEMBL204656 YesY
NIAID ChemDB 241767
Chemical data
Formula C23H23ClFNO5 
Mol. mass 447.883 g/mol
 N (what is this?)  (verify)

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 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]

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.[6]

References[edit]

  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. doi:10.1128/JVI.01534-07. PMC 2224569. PMID 17977962. 
  4. ^ 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. 
  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. doi:10.1016/S0140-6736(12)60917-9. PMID 22748591.  edit
  6. ^ 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.