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Inhibitory effect of 5-fluorouracil on human cytochrome P450 isoforms in human liver microsomes

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

Objective

A number of case reports have been described regarding drug interactions with 5-fluorouracil (5-FU) and co-administered drugs. However, little is known regarding the inhibitory potential of 5-FU on the metabolism of co-administered drugs by cytochrome P 450 (CYP). The aim of the present study was to elucidate the inhibitory effect of 5-FU on CYP isoforms using human liver microsomes.

Methods

The inhibitory effect of 5-FU on CYP1A2, CYP2C9, CYP2C19, CYP2C8, CYP2E1, CYP2D6, and CYP3A4 activities was examined with specific probe drugs in human liver microsomes.

Results

5-FU showed little or no inhibitory effect on CYP-catalyzed reactions in human liver microsomal preparations.

Conclusion

5-FU has no inhibitory effect on CYP isoforms or drug metabolism causing drug interaction with 5-FU. The mechanism that causes drug interaction between co-administered drugs and 5-FU may not be related to direct CYP inhibition by 5-FU.

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Authors and Affiliations

  1. Department of Pharmacology, Gachon Medical School, 1198 Kuwol-dong, Namdong-gu, 405–760 , Incheon, Korea

    Ji-Young Park

  2. East West Medical Research Institute, Kyung Hee University, Seoul, Korea

    Kyoung-Ah Kim

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  1. Ji-Young Park
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  2. Kyoung-Ah Kim
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Correspondence to Ji-Young Park.

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Park, JY., Kim, KA. Inhibitory effect of 5-fluorouracil on human cytochrome P450 isoforms in human liver microsomes. Eur J Clin Pharmacol 59, 407–409 (2003). https://doi.org/10.1007/s00228-003-0641-z

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  • DOI: https://doi.org/10.1007/s00228-003-0641-z

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