Monograph
M04AA03 - Febuxostat |
Propably not porphyrinogenic |
PNP |
Rationale
Febuxostat is a substrate of CYP 1A1, 1A2, 2C8 and 2C9, but it has not shown potential for significant induction or inhibition of CYP enzymes. No potentially porphyrinogenic pharmacokinetic properties are suspected.
Chemical description
Febuxostat is a thiazole derivative and inhibitor of xanthine oxidase.
Therapeutic characteristics
Febuxostat is used in the treatment of chronic hyperuricaemia. It is administered orally and has a half-life of approximately 5 to 8 hours.
Metabolism and pharmacokinetics
The metabolism of febuxostat includes oxidation by CYP1A1, CYP1A2, CYP2C8 or CYP2C9 into at least three active metabolites. (SPC, Adenuric)
In an in vitro study of potential drug-drug interactions including testing for possible interactions with CYP1A1, 2C9, 2C19, 2D6, and 3A4, only weak inhibition of CYP 2D6 was shown (Mukoyoshi 2008).
According to the SPC, in vitro studies have shown potential for CYP 2C8 and 2D6 inhibition. In vivo studies found no effect on CYP 2C8 and only negligible inhibition of CYP 2D6.
No potential CYP interactions are listed in drug-drug- interaction databases. (Lexi-interact, NOMA, The Danish Health and Medicines Authority).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | In vitro drug-drug interaction studies with febuxostat, a novel non-purine selective inhibitor of xanthine oxidase: plasma protein binding, identification of metabolic enzymes and cytochrome P450 inhibition.
Mukoyoshi M, Nishimura S et al. Xenobiotica. 2008 May;38(5):496-510. |
18421623 |
| * | Government bodies | |
| 2. | Norwegian medicines agency (NOMA). Find medicine.
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| * | Drug interaction databases | |
| 3. | Lexi-Interact, via UpToDate.
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| 4. | The Danish Health and Medicines Authority. The drug interaction database.
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| * | Summary of Product Characteristics | |
| 5. | European Medicines Agency, SPC Adenuric (
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