News and Commentary
The Pharmacogenomics Journal , (4 October 2016) | doi:10.1038/tpj.2016.73
Tamoxifen metabolism in breast cancer treatment: Taking the focus off the CYP2D6 gene
A Novillo, A Romero-Lorca, M Gaibar, M Rubio and A Fernández-Santander
Abstract
Tamoxifen (TAM) has been widely used to treat estrogen receptor (ER)-positive breast cancer, and has led to reduction of 50% in the annual recurrence rate and 30% in breast cancer mortality after 5 years of treatment.1 The prodrug TAM is a selective ER modulator that antagonizes ERs in cancer cells. However, compared with its two active metabolites 4-hydroxy-TAM (4-OH-TAM) and endoxifen, it is a relatively weak antiestrogen.
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