A key step forward in the treatment of hor- mone-dependent diseases has been made since the discovery of tissue-speci c steroid receptor modulators (SRMs), or receptor lig- ands that elicit agonistic or antagonistic ef- fects in a cell- and tissue-dependent manner. In reproductive medicine, selective estrogen receptors modulators (SERMs) and selective progesterone receptors modulator (SPRMs) were discovered and developed since the 1970s. SERMs were rst released for the treatment of infertility and later developed in areas such as osteoporosis prevention and breast cancer treatment. The later dis- covery of SPRMs has provided molecules active on the inhibition of ovulation, on the endometrium and on leiomyoma cells, which are currently being developed for their anti- proliferative effects in breast cancer and en- dometriosis. New molecules and new routes of administration of SERMs and SPRMs are in development for cancer treatment, long-term contraception and endometriosis. Based on the future advancements on the understand- ing of the mechanisms of action of these compounds, it is to be expected that future SRMs will emerge for newer indications.
Selective steroid receptor modulators in reproductive medicine.
GIANNINI, ANDREA;RUSSO, ELEONORA;MANNELLA, PAOLO;SIMONCINI, TOMMASO
2015-01-01
Abstract
A key step forward in the treatment of hor- mone-dependent diseases has been made since the discovery of tissue-speci c steroid receptor modulators (SRMs), or receptor lig- ands that elicit agonistic or antagonistic ef- fects in a cell- and tissue-dependent manner. In reproductive medicine, selective estrogen receptors modulators (SERMs) and selective progesterone receptors modulator (SPRMs) were discovered and developed since the 1970s. SERMs were rst released for the treatment of infertility and later developed in areas such as osteoporosis prevention and breast cancer treatment. The later dis- covery of SPRMs has provided molecules active on the inhibition of ovulation, on the endometrium and on leiomyoma cells, which are currently being developed for their anti- proliferative effects in breast cancer and en- dometriosis. New molecules and new routes of administration of SERMs and SPRMs are in development for cancer treatment, long-term contraception and endometriosis. Based on the future advancements on the understand- ing of the mechanisms of action of these compounds, it is to be expected that future SRMs will emerge for newer indications.File | Dimensione | Formato | |
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