Article
Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen.
Breast cancer research and treatment - 1 May 2004
Johnson Michael D, Zuo Hong, Lee Kyung-Hoon, Trebley Joseph P, Rae James Michael, Weatherman Ross V, Desta Zeruesanay, Flockhart David A, Skaar Todd C
Abstract excerpt
The antiestrogen tamoxifen is extensively metabolized in patients to form a series of compounds with altered affinity for estrogen receptors (ERs), the primary target of this drug. Furthermore, these metabolites exhibit a range of partial agonist and antagonist activities for ER mediated effects that do not depend directly on their absolute affinity for ERs. Thus, clinical response to tamoxifen therapy is likely...
Topics
- Breast Neoplasms
- Cell Division
- Cytochrome P-450 CYP2D6
- Drug Interactions
- Female
- Genotype
- Humans
- Receptors, Estrogen
- Tamoxifen
- Tumor Cells, Cultured