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How is tamoxifen excreted? Tamoxifen itself is a prodrug is metabolized in the liver by the cytochrome P450 isoforms CYP3A4, CYP2C9, and CYP2D6 into active metabolites such as afimoxifene and endoxifen. Tamoxifen and its metabolites undergo conjugation, including glucuronidation and sulfation. Tamoxifen may inhibit its own metabolism.

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