Selective estrogen receptor modulators (SERM) : new substances for hormone replacement therapy
Burckhardt, P.
Schweizerische Medizinische Wochenschrift 129(49): 1926-1930
1999
ISSN/ISBN: 0036-7672 PMID: 10635085 Document Number: 509161
The term "SERM" stands for "Selective Estrogen Receptor Modulators", substances which act on certain organs as oestrogen agonists and on other organs as oestrogen antagonists. They can exert the known oestrogen-like effects on bone and lipids without exerting any action on the endometrium and the breast, a potentially ideal profile for postmenopausal hormone replacement treatment. Long known are clomifen, an ovulation stimulator, and tamoxifen, used for secondary prevention in breast cancer. Tamoxifen prevents postmenopausal bone loss as efficiently as hormone replacement treatment, and lowers blood lipids and the coronary risk, but increases the risk of endometrial cancer; for this reason it cannot be used in the prevention of postmenopausal osteoporosis. Raloxifen stimulates neither the endometrium nor the mammary gland, and probably even lowers the risk of breast cancer. Its relatively mild but significant effect on BMD (+ 2-3%/2 years) is sufficient for prevention, and in osteoporotics goes along with a substantial decrease in vertebral fracture incidence (by about 50%) comparable to the effect of other treatments. As in hormone replacement treatment, thromboembolism and leg cramps occur more frequently. Therefore, raloxifen can be used in women free of climacteric symptoms for the prevention and treatment of postmenopausal osteoporosis with no increased risk of phlebitis, alone or in combination with calcium, vitamin D, bisphosphonates and calcitonin; in future it may also be useful in male osteoporosis.