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Background <p>Resveratrol is a natural compound and commonly used dietary supplement, especially for its anticancer properties. However, there is a lack of pharmacokinetic (PK) studies investigating its interactions with anticancer drugs, including tyrosine kinase inhibitors (TKIs). This study aimed to investigate the effect of resveratrol on erlotinib pharmacokinetics, a TKI indicated for non-small-cell lung cancer (NSCLC). Another aim was to develop and validate a new high-performance liquid chromatography with fluorescence detection (HPLC-FLD) method as a simple and cost-effective assay to quantify erlotinib levels in rat plasma in vivo.</p> Methods <p>HPLC-FLD was used to develop and validate a method for quantifying erlotinib in rat plasma. A PK study was conducted with four groups of male Sprague–Dawley rats: erlotinib (20&#xa0;mg/kg) alone, erlotinib with either single or multiple doses of resveratrol (100&#xa0;mg/kg), and a control group. Blood samples were collected and analyzed by HPLC-FLD, and the PK parameters were estimated.</p> Results <p>A 4-min runtime HPLC-FLD method was developed and validated. Single and multiple doses of resveratrol significantly increased the total area under the curve <InlineEquation ID="IEq2"> <EquationSource Format="TEX">\({\text{AUC}}_{0}^{\infty }\)</EquationSource> <EquationSource Format="MATHML"><math> <msubsup> <mtext>AUC</mtext> <mrow> <mn>0</mn> </mrow> <mi>∞</mi> </msubsup> </math></EquationSource> </InlineEquation>, by approximately 2- and 3-fold, respectively, while both decreased the clearance (Cl/F) of erlotinib by approximately 2-fold.</p> Conclusion <p>Resveratrol, even at a single dose, can alter erlotinib pharmacokinetics which may cause clinically relevant drug interactions, particularly considering erlotinib significant interindividual variability and narrow therapeutic index. The new HPLC-FLD method is a reliable, simple, and cost-effective assay that can be used in erlotinib PK studies and therapeutic drug monitoring.</p>

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Resveratrol alters erlotinib pharmacokinetics in rats: application of a rapid HPLC-fluorescence method for quantifying erlotinib in plasma

  • 期刊论文

  • 发表日期：

    2025年7月2日

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  • Aref L. Zayed,
  • Jomana Al. Hroot,
  • Ruba S. Darweesh,
  • Nidal A. Qinna,
  • Aysheh M. Alshekhhossin,
  • Omar M. Al Kilani

摘要

Background

Resveratrol is a natural compound and commonly used dietary supplement, especially for its anticancer properties. However, there is a lack of pharmacokinetic (PK) studies investigating its interactions with anticancer drugs, including tyrosine kinase inhibitors (TKIs). This study aimed to investigate the effect of resveratrol on erlotinib pharmacokinetics, a TKI indicated for non-small-cell lung cancer (NSCLC). Another aim was to develop and validate a new high-performance liquid chromatography with fluorescence detection (HPLC-FLD) method as a simple and cost-effective assay to quantify erlotinib levels in rat plasma in vivo.

Methods

HPLC-FLD was used to develop and validate a method for quantifying erlotinib in rat plasma. A PK study was conducted with four groups of male Sprague–Dawley rats: erlotinib (20 mg/kg) alone, erlotinib with either single or multiple doses of resveratrol (100 mg/kg), and a control group. Blood samples were collected and analyzed by HPLC-FLD, and the PK parameters were estimated.

Results

A 4-min runtime HPLC-FLD method was developed and validated. Single and multiple doses of resveratrol significantly increased the total area under the curve \({\text{AUC}}_{0}^{\infty }\) AUC 0 ∞ , by approximately 2- and 3-fold, respectively, while both decreased the clearance (Cl/F) of erlotinib by approximately 2-fold.

Conclusion

Resveratrol, even at a single dose, can alter erlotinib pharmacokinetics which may cause clinically relevant drug interactions, particularly considering erlotinib significant interindividual variability and narrow therapeutic index. The new HPLC-FLD method is a reliable, simple, and cost-effective assay that can be used in erlotinib PK studies and therapeutic drug monitoring.