Tamoxifen pharmacogenomics: The role of CYP2D6 as a predictor of drug response

M. P. Goetz, A. Kamal, M. M. Ames

Research output: Contribution to journalReview articlepeer-review

152 Scopus citations


Tamoxifen continues to be a standard endocrine therapy for the prevention and treatment of estrogen receptor (ER)-positive breast cancer. Tamoxifen can be considered a classic "pro-drug," requiring metabolic activation to elicit pharmacological activity. CYP2D6 is the rate-limiting enzyme catalyzing the conversion of tamoxifen into metabolites with significantly greater affinity for the ER and greater ability to inhibit cell proliferation. Both genetic and environmental (drug-induced) factors that alter CYP2D6 enzyme activity directly affect the concentrations of the active tamoxifen metabolites and the outcomes of patients receiving adjuvant tamoxifen. The a priori knowledge of the pharmacogenetic variation known to abrogate CYP2D6 enzyme activity may provide a means by which the hormonal therapy of breast cancer can be individualized.

Original languageEnglish (US)
Pages (from-to)160-166
Number of pages7
JournalClinical pharmacology and therapeutics
Issue number1
StatePublished - Jan 9 2008

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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