Estrogen-Receptor Binding Mode Raloxifene

Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women. It was announced on April 17, 2006, that raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in certain high risk groups of females, though with a reduced risk of thromboembolic events and cataracts in patients taking raloxifene versus those taking tamoxifen. On September 14, 2007, the U.S. Food and Drug Administration announced approval of raloxifene for reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.

There has been criticism in the mainstream oncology press of the way that information about the drug was released.There has been some confusion in the lay media about the meaning of the trial results. There is no specific clinical evidence for the use of raloxifene in the adjuvant treatment of breast cancer over established drugs such as tamoxifen or anastrozole.

Pharmacogenomic Testing and Breast Cancer

Genomic heterogeneity is emerging as an important factor in determining tamoxifen benefit in breast cancer. Dr. Hannah Linden, Associate Professor of Medicine at the University of Washington, and a breast cancer oncologist at the SCCA and HMC will review recent laboratory and clinical trial evidence regarding tamoxifen metabolism and the impact of CYP2D6 pharacogenomic profiling.

 

About Tamoxifen

Tamoxifen is an orally taken selective estrogen receptor modulator (SERM) that is used in the treatment of breast cancer and is currently the world's largest selling drug for that purpose.Tamoxifen was discovered by ICI Pharmaceuticals(now AstraZeneca) and is sold under the trade names Nolvadex, Istubal, and Valodex. However, the drug, even before its patent expiration, was and still is widely referred to by its generic name "tamoxifen."

Tamoxifen is currently used for the treatment of both early and advanced ER+ (estrogen receptor positive) breast cancer in pre- and post-menopausal women.It is also approved by the FDA for the prevention of breast cancer in women at high risk of developing the disease.It has been further approved for the reduction of contralateral (in the opposite breast) cancer.



About Speaker
Dr. Linden received her MD from the University of Massachusetts, Amherst, MA. She completed her Internal Medicine Residency at the University of Arizona, Tuscon, AZ. She was a Post-Doctoral Fellow in Hematology at the University of Washington, Seattle, WA.