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An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma.

Liying Xing1, Ya-Nan Liu2, Hongye Yao1

  • 1The First People's Hospital of Jiashan, Jiaxing, China.

Frontiers in Pharmacology
|July 5, 2022
PubMed
Summary

Daidzein may affect how the body processes relugolix, a medication for endometriosis. This study explored their interaction, finding daidzein potentially speeds up relugolix metabolism, though not statistically significant.

Keywords:
GnRH antagonistdaidzeinendometriosisrelugolixuterine fibroids

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Analytical Chemistry

Background:

  • Relugolix is a GnRH receptor antagonist used for endometriosis.
  • Relugolix is primarily metabolized by CYP3A4 enzymes.
  • Daidzein is known to induce CYP3A4 enzyme activity.

Purpose of the Study:

  • To investigate the pharmacokinetic interaction between daidzein and relugolix in rats.
  • To develop and validate an UPLC-MS/MS method for quantifying relugolix in biological matrices.

Main Methods:

  • An ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was developed and validated.
  • Rats were administered relugolix alone or in combination with daidzein.
  • Pharmacokinetic parameters of relugolix were analyzed.

Main Results:

  • The UPLC-MS/MS method demonstrated excellent linearity, precision, accuracy, stability, and recovery.
  • Co-administration of daidzein resulted in a decrease in relugolix's Cmax (15.56%) and AUC0-t (21.36%).
  • These changes suggest a trend of daidzein inducing relugolix metabolism, indicating a potential food-drug interaction.

Conclusions:

  • Daidzein may influence the metabolism of relugolix.
  • The developed UPLC-MS/MS method is suitable for pharmacokinetic studies.
  • Further research is warranted to fully elucidate the clinical significance of this interaction.