The effect of β-carotene supplementation on the pharmacokinetics of nelfinavir and its active metabolite M8 in HIV-1-infected patients

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

*Corresponding author for this work

Research output: Contribution to journalArticle

9 Citations (Scopus)

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 (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.

Original languageEnglish
Pages (from-to)688-702
Number of pages15
JournalMolecules
Volume17
Issue number1
DOIs
Publication statusPublished - Jan 2012

Keywords

  • β-carotene
  • HIV
  • Interaction
  • Nelfinavir
  • Pharmacokinetics

ASJC Scopus subject areas

  • Organic Chemistry

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