Abstract: β-Carotene supplements are often taken by individuals living with HIV-1. Contradictory results from in vitro studies suggest that β-carotene may inhibit or induce cytochrome P450 enzymes and transporters. The study objective was to investigate the effect of β-carotene on the steady-state pharmacokinetics of nelfinavir and its active metabolite M8 in HIV-1 infected individuals. Twelve hour nelfinavir pharmacokinetic analysis was conducted at baseline and after 28 days of β-carotene supplementation (25,000 IU twice daily). Nelfinavir and M8 concentrations were measured with validated assays. Non-compartmental methods were used to calculate the pharmacokinetic parameters. Geometric mean ratios comparing day 28 to day 1 area under the plasma concentration-time curve (AUC0–12 h), maximum (Cmax) and minimum (Cmin) concentrations of nelfinavir and M8 are presented with 90% confidence intervals. Eleven subjects completed the study and were included in the analysis. There were no significant differences in nelfinavir AUC0–12 h and Cmin (−10%, +4%) after β-carotene supplementation. The M8 Cmin was increased by 31% while the M8 AUC0–12 h and Cmax were unchanged. During the 28 day period, mean CD4+ % and CD4+:CD8+ ratio increased significantly (p < 0.01). β-carotene supplementation increased serum carotene levels but did not cause any clinically significant difference in the nelfinavir and M8 exposure.
Keywords: β-carotene; HIV; nelfinavir; interaction; pharmacokinetics
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Sheehan, N.L.; Heeswijk, R.P.G.; Foster, B.C.; Akhtar, H.; Singhal, N.; Seguin, I.; DelBalso, L.; Bourbeau, M.; Chauhan, B.M.; Boulassel, M.-R.; Burger, D.M.; Lalonde, R.G.; Cameron, D.W. The Effect of β-Carotene Supplementation on the Pharmacokinetics of Nelfinavir and Its Active Metabolite M8 in HIV-1-infected Patients. Molecules 2012, 17, 688-702.
Sheehan NL, Heeswijk RPG, Foster BC, Akhtar H, Singhal N, Seguin I, DelBalso L, Bourbeau M, Chauhan BM, Boulassel M-R, Burger DM, Lalonde RG, Cameron DW. The Effect of β-Carotene Supplementation on the Pharmacokinetics of Nelfinavir and Its Active Metabolite M8 in HIV-1-infected Patients. Molecules. 2012; 17(1):688-702.
Sheehan, Nancy L.; Heeswijk, Rolf P. G. van; Foster, Brian C.; Akhtar, Humayoun; Singhal, Neera; Seguin, Isabelle; DelBalso, Lina; Bourbeau, Marc; Chauhan, Bobby M.; Boulassel, Mohammed-Rachid; Burger, David M.; Lalonde, Richard G.; Cameron, Donald William. 2012. "The Effect of β-Carotene Supplementation on the Pharmacokinetics of Nelfinavir and Its Active Metabolite M8 in HIV-1-infected Patients." Molecules 17, no. 1: 688-702.