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

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

    Fingerprint

Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Sheehan, N. L., Van 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. (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