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Molecules 2012, 17(1), 688-702; doi:10.3390/molecules17010688
Article

The Effect of β-Carotene Supplementation on the Pharmacokinetics of Nelfinavir and Its Active Metabolite M8 in HIV-1-infected Patients

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Received: 9 December 2011 / Revised: 5 January 2012 / Accepted: 6 January 2012 / Published: 12 January 2012
(This article belongs to the Special Issue Carotenoids)
Download PDF [285 KB, 18 June 2014; original version 18 June 2014]

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 β-carotene; HIV; nelfinavir; interaction; pharmacokinetics
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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