Molecules (Jan 2012)

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

  • Humayoun Akhtar,
  • Neera Singhal,
  • Isabelle Seguin,
  • Lina DelBalso,
  • Marc Bourbeau,
  • Bobby M. Chauhan,
  • Donald William Cameron,
  • Mohammed-Rachid Boulassel,
  • David M. Burger,
  • Richard G. Lalonde,
  • Nancy L. Sheehan,
  • Rolf P. G. van Heeswijk,
  • Brian C. Foster

DOI
https://doi.org/10.3390/molecules17010688
Journal volume & issue
Vol. 17, no. 1
pp. 688 – 702

Abstract

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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.

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