The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen by Goetz Matthew P, Knox Stacey K, Suman Vera J, Rae James M, Safgren Stephanie L, Ames Matthew M, Visscher Daniel W, Reynolds Carol, Couch Fergus J, Lingle Wilma L, Weinshilboum Richard M, Fritcher Emily G Barr, Nibbe Andrea M, Desta Zeruesenay, Nguyen Anne, Flockhart David A, Perez Edith A, Ingle James N in Breast cancer research and treatment (2007).

[PMID: 17115111] PubMed


Tamoxifen is biotransformed to the potent anti-estrogen, endoxifen, by the cytochrome P450 (CYP) 2D6 enzyme. CYP2D6 genetic variation and inhibitors of the enzyme markedly reduce endoxifen plasma concentrations in tamoxifen-treated patients. Using a North Central Cancer Treatment Group adjuvant tamoxifen trial, we performed a comprehensive evaluation of CYP2D6 metabolism by assessing the combined effect of genetic variation and inhibition of the enzyme system on breast cancer recurrence and death.

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