TY - JOUR
T1 - The evolution of tamoxifen therapy in breast cancer
T2 - Selective oestrogen-receptor modulators and downregulators
AU - O'Regan, Ruth M.
AU - Jordan, V. Craig
N1 - Funding Information:
The authors are supported by the Lynn Sage Breast Cancer Foundation of Northwestern Memorial Hospital, a National Surgical Adjuvant Breast and Bowel Project Clinical Young Investigator Award, Avon Healthcare Foundation, and a SPORE grant in breast cancer (CA 89018-01). We thank James Zapf (MAXIA Pharmaceuticals Inc, San Diego, CA, USA) for providing the computer modeling of the SERM-ER complexes.
PY - 2002
Y1 - 2002
N2 - Tamoxifen is the most widely used hormonal treatment for all stages of breast cancer and has been approved for the prevention of breast cancer in high-risk women. The observation that tamoxifen acts as an antioestrogen on the breast but has paradoxical oestrogenic effects on bones and lipids heralded the development of the selective oestrogen-receptor modulators (SERM). Raloxifene, another of these drugs, is being used to prevent osteoporosis in postmenopausal women, but it seems, like tamoxifen, to prevent breast cancer. The molecular basis for these target-site-specific actions remains unclear but may involve the relative expressions of coregulatory proteins in target tissues. Several new SERM agents are in clinical development in an attempt to decrease the unwanted effects. Furthermore, two different classes of hormonal agents, the aromatase inhibitors and oestrogen-receptor downregulators, which have no oestrogen-like properties at any site, are promising new treatments for breast cancer.
AB - Tamoxifen is the most widely used hormonal treatment for all stages of breast cancer and has been approved for the prevention of breast cancer in high-risk women. The observation that tamoxifen acts as an antioestrogen on the breast but has paradoxical oestrogenic effects on bones and lipids heralded the development of the selective oestrogen-receptor modulators (SERM). Raloxifene, another of these drugs, is being used to prevent osteoporosis in postmenopausal women, but it seems, like tamoxifen, to prevent breast cancer. The molecular basis for these target-site-specific actions remains unclear but may involve the relative expressions of coregulatory proteins in target tissues. Several new SERM agents are in clinical development in an attempt to decrease the unwanted effects. Furthermore, two different classes of hormonal agents, the aromatase inhibitors and oestrogen-receptor downregulators, which have no oestrogen-like properties at any site, are promising new treatments for breast cancer.
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U2 - 10.1016/S1470-2045(02)00711-8
DO - 10.1016/S1470-2045(02)00711-8
M3 - Review article
C2 - 12067682
AN - SCOPUS:0036232065
SN - 1470-2045
VL - 3
SP - 207
EP - 214
JO - Lancet Oncology
JF - Lancet Oncology
IS - 4
ER -