Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response.
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.
Duke Scholars
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- Treatment Outcome
- Tamoxifen
- Phenotype
- Pharmacology & Pharmacy
- Pharmacogenetics
- Patient Selection
- Humans
- Genotype
- Genetic Variation
- Female
Citation
Published In
DOI
EISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- Treatment Outcome
- Tamoxifen
- Phenotype
- Pharmacology & Pharmacy
- Pharmacogenetics
- Patient Selection
- Humans
- Genotype
- Genetic Variation
- Female