Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response.

Journal Article (Journal Article;Review)

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.

Full Text

Duke Authors

Cited Authors

  • Goetz, MP; Kamal, A; Ames, MM

Published Date

  • January 2008

Published In

Volume / Issue

  • 83 / 1

Start / End Page

  • 160 - 166

PubMed ID

  • 17882159

Pubmed Central ID

  • PMC2752373

Electronic International Standard Serial Number (EISSN)

  • 1532-6535

Digital Object Identifier (DOI)

  • 10.1038/sj.clpt.6100367


  • eng

Conference Location

  • United States