from Wiktionary, Creative Commons Attribution/Share-Alike License

  • n. The metabolic activation of xenobiotic compounds into reactive, toxic compounds


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  • Blood leaving the liver is eventually distributed to all other areas of the body; however, much of the absorbed xenobiotic has undergone detoxication or bioactivation.


  • There are two types of metabolism - detoxification and bioactivation.


  • To characterise whether some selective serotonin reuptake inhibitor (SSRI) antidepressants reduce tamoxifen's effectiveness by inhibiting its bioactivation by cytochrome P450 2D6 (CYP2D6).

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  • Steinkellner H, Rabot S, Freywald C, et al. Effects of cruciferous vegetables and their constituents on drug metabolizing enzymes involved in the bioactivation of DNA-reactive dietary carcinogens.

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  • The cytochrome P450 (CYP) gene family catalyzes drug metabolism and bioactivation and is therefore relevant to drug development.

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  • 2 The bioactivation of tamoxifen to endoxifen is mainly catalysed by the cytochrome P450 isoenzyme 2D6 (CYP2D6) .2

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