[Selective estrogen receptor modulators (SERMs) in the practice].
Selective estrogen receptor modulators (SERMs) represent a growing class of compounds that act as either estrogen receptor gonists or ntagonists in tissue-selective manner. SERMs with the appropriate selectivity profile offer the opportunity to dissociate the favorable bone and cardio-vascular effects of estrogen from its unfavorable stimulatory effects on the breast and uterus. The triphenylethylene drug tamoxifen proved to be invaluable to treat and protect against breast cancer and bone loss, probably reduces cardiovascular risk, but had side effects on uterus similar to natural estrogens. The tamoxifen derivate toremifene is also used to treat breast cancer, but has less effect on bone. The non-steroidal benzothiophene derivate, raloxifene, is the best SERM available thus far. It has the potential to prevent breast cancer (like tamoxifen), but has better profile in its actions on bone and cardiovascular system (produces a rapid reduction of serum cholesterol, decreases fibrinogen and lipoprotein, improves the vascular epithelial function, attenuates vascular intimal thickening, etc.). It does not increase the incidence of endometrial cancer. Compounds of this class are the first step in developing the perfect hormone replacement and other multitargeted therapy. This review summarizes the recent important knowledge about SERMs.
Nagykálnai
Tamás
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Onkoradiológiai Központ, Fôvárosi Onkormányzat Uzsoki utcai Kórház, Budapest, 1145, Hungary.
D001943:Breast Neoplasms / Q000517:prevention & control*; D003327:Coronary Disease / Q000517:prevention & control*; D004965:Estrogen Antagonists / Q000494:pharmacology; D004967:Estrogens / Q000819:agonists; D005260:Female; D006801:Humans; D015663:Osteoporosis, Postmenopausal / Q000517:prevention & control*; D020849:Raloxifene Hydrochloride / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000187:drug effects*; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology* / Q000627:therapeutic use*; D013629:Tamoxifen / Q000494:pharmacology; D017312:Toremifene / Q000494:pharmacology
D004965:Estrogen Antagonists; D004967:Estrogens; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen; D020849:Raloxifene Hydrochloride; D017312:Toremifene