Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: implication for optimization of breast cancer treatment by Borges Silvana, Desta Zeruesenay, Li Lang, Skaar Todd C, Ward Bryan A, Nguyen Anne, Jin Yan, Storniolo Anna Maria, Nikoloff D Michele, Wu Lin, Hillman Grant, Hayes Daniel F, Stearns Vered, Flockhart David A in Clinical pharmacology and therapeutics (2006).

[PMID: 16815318] PubMed


N-Desmethyltamoxifen (NDM), a major primary metabolite of tamoxifen, is hydroxylated by cytochrome P450 (CYP) 2D6 to yield endoxifen. Because of its high antiestrogenic potency, endoxifen may play an important role in the clinical activity of tamoxifen. We conducted a prospective trial in 158 patients with breast cancer who were taking tamoxifen to further understand the effect of CYP2D6 genotype and concomitant medications on endoxifen plasma concentrations.

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