ABSTRACT
Elvitegravir (GS-9137, JTK-303, Vitekta, marketed by Gilead) is a dihydroquinoline carboxylic acid that exhibits the active, integrase inhibitor conferring beta-hydroxy-ketone structural motif. The chemical structure of elvitegravir is shown in Figure 250.1. Like raltegravir and dolutegravir, elvitegravir is a specific inhibitor of the strand transfer step of HIV integration (DeJesus et al., 2006). As a result, these related molecules are often referred to as strand-transfer inhibitors. In vitro experiments approximate elvitegravir to be greater than two times more potent than raltegravir against HIV-1 integrase-mediated strand transfer (Marinello et al., 2008). Elvitegravir was approved in 2012 as a fixed-dose combination with cobicistat (a pharmacokinetic booster) and emtricitabine and tenofovir disoproxil fumarate (Stribild, Gilead Sciences) as initial therapy for treatment-naive patients with HIV/AIDS (FDA, 2012). In 2014, the FDA approved elvitegravir (Vitekta, Gilead Sciences) as an individual drug to be used in combination with ritonavir-boosted protease inhibitor plus other antiretrovirals for treatment-experienced HIV-positive adults although this has since been discontinued by the manufacturer (FDA, 2014a; Gilead, 201). In 2015, the FDA approved the fixed-dose combination of elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide (Genvoya, Gilead Sciences) for the initial treatment of HIV-1 infection in adults and pediatric patients 12 years of age and to replace current antiretroviral regimens in patients with at least 6 months of virologic suppression (FDA, 2015). The chemical structure of elvitegravir (EVG, GS-9137, JTK-303). https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig250_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>
