icon-folder.gif   Conference Reports for NATAP  
  49th ICAAC
San Francisco, CA
September 12-15, 2009
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Effect of Food on Pharmacokinetics of Elvitegravir, Emtricitabine, Tenofovir DF and the Pharmacoenhancer GS-9350 as a Fixed- Dose Combination Tablet
  Reported by Jules Levin
ICAAC Sept 11-15 2009 San Francisco
P German,1 D Warren,1 L Wei,1 L Zhong,1 J Hui,2 and BP Kearney1 1Gilead Sciences, Inc., Foster City, CA, USA; 2Gilead Sciences, Inc., Durham, NC, USA
Gilead's investigational HIV-1 integrase inhibitor, elvitegravir (EVG), is primarily metabolized by CYP3A enzymes
GS-9350 lacks antiretroviral activity and is in development as a pharmacoenhancer (booster) to increase the systemic levels of coadministered CYP3A substrates, such as EVG and HIV protease inhibitors (PIs)
GS-9350 may be an alternative to ritonavir (RTV) as the pharmacoenhancer of EVG
Administration of a single unboosted 400 mg EVG dose results in Cmax and AUCinf increases of 3.3-fold and 2.7-fold, respectively in the fed (575 kcal, 33% fat) versus fasted state1
The current dosing recommendation for RTV-boosted EVG is administration with a meal to improve pharmacokinetics (PK) and tolerability and due to its concurrent administration with RTV-boosted PIs