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 (AUC 0-12 h), maximum (C max) and minimum (C min) 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 and C min (-10%, +4%) after β-carotene supplementation. The M8 C min was increased by 31% while the M8 AUC 0-12 h and C max 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. © 2012 by the authors.
CITATION STYLE
Sheehan, N. L., Van Heeswijk, R. P. G., Foster, B. C., Akhtar, H., Singhal, N., Seguin, I., … Cameron, D. W. (2012). The effect of β-carotene supplementation on the pharmacokinetics of nelfinavir and its active metabolite M8 in HIV-1-infected patients. Molecules, 17(1), 688–702. https://doi.org/10.3390/molecules17010688
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