The pharmacokinetic profile of raltegravir-containing antiretroviral therapy in HIV-infected individuals over 60 years of age. Issue 1 (February 2015)

• Record Type: Journal Article
• Authors: Vera, Jaime H.; Jackson, Akil; Dickinson, Laura; Else, Laura; Barber, Tristan; Mora-Peris, Borja; Back, David; Boffito, Marta; Winston, Alan
• Is Part Of: HIV clinical trials. Volume 16:Issue 1(2015)
• Page Start: 39
• Page End: 42
• Publication Date: 2015-02
• Subjects: Raltegravir, -- Pharmacokinetics, -- Aging; HIV Infections -- Chemotherapy -- Periodicals; AIDS (Disease) -- Chemotherapy -- Periodicals; HIV Infections -- Research -- Periodicals; AIDS (Disease) -- Research -- Periodicals; 616.979206105
• DOI: 10.1179/1528433614Z.0000000006
• Languages: English
• ISSNs: 1528-4336

Abstract

Abstract : Background: Antiretroviral safety and efficacy and may differ in older versus younger HIV-infected patients. The objective of this study was to assess the pharmacokinetic (PK) profile in older HIV-infected subjects (>60 years) switching combination antiretroviral therapy (cART) to a raltegravir (RAL) containing regimen. Methods: Nineteen HIV-infected patients over 60 years of age on effective cART (HIV-RNA < 50 copies/ml) were enrolled in this prospective 24-week study. On day 1, patients switched to tenofovir/emtricitabine (245/200 mg once daily) and RAL (400 mg twice daily). On day 28, intensive PK sampling was undertaken in a fasted state and RAL plasma concentrations determined. Neurocognitive function was assessed at baseline and week 24 using a neuropsychological battery. RAL PK parameters were compared to those of two younger historical HIV-infected control groups that received twice-daily RAL co-administered with darunavir/ritonavir (DRV/r) 800/100 once daily by nonlinear mixed effects modelling. Results: In HIV-infected subjects over the age of 60 (mean ± SD age: 66 ± 3.4 years, n = 19) switching to a RAL containing regimen, we observed no safety concerns, no plasma virological rebounds, and no differences in RAL apparent oral clearance when compared to younger HIV-infected populations (mean ± SD age: 41 ± 9.2 years, n = 38) based on population pharmacokinetic analysis. After 24 weeks of study therapy a decline in cognitive function was observed [change in (SD) global score of (0.91 (1.3), P = 0.018]. Conclusions: No significant changes in RAL exposure associated with age were observed.