Selective estrogen receptor modulator

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Selective estrogen receptor modulators ( SERM ) are medicinal substances that mediate their effect via estrogen receptors . They belong to the group of antiestrogens .

The selective estrogen receptor modulators are chemically different compounds that do not have a steroid structure like the estrogens . These include clomifene , raloxifene , tamoxifene , toremifene , bazedoxifene , lasofoxifene and ormeloxifene . These substances are used in particular in the treatment of female infertility , breast cancer , osteoporosis and endometriosis .

Ormeloxifene has been marketed successfully as a hormone-free anti-baby pill under the brand name Saheli since 1992. Taken once a week, the Pearl Index is <2, as it prevents the fertilized egg cell from implanting.

It has been known for some time that the substances used do not inhibit all estrogen receptors. A distinction is made between the alpha (ERα) and beta (ERβ) types of estrogen receptors. The ERα receptors are found in the breast, uterus , pituitary gland and hypothalamus . The ERβ receptors, on the other hand, are found in the bones, vessels, hippocampus and higher centers of the central nervous system. Raloxifene inhibits z. B. the ERα receptors and at the same time stimulates the ERβ receptors, so that breast cancer growth is inhibited without negating the protective estrogen effect on the bones. That is why one speaks of selective estrogen receptor modulators.

Also compare antiandrogens

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  1. Riggs, BL & Hartmann, LC (2003): Selective estrogen-receptor modulators -mechanisms of action and application to clinical practice . In: N. Engl. J. Med. Vol. 348, pp. 618-629. PMID 12584371
  2. ^ Saheli - the only non-hormonal birth control pill. Retrieved April 21, 2020 (English).