Antiestrogen

Antiestrogens (also called estrogen blockers ) are drugs that inhibit the effects of the female sex hormone estrogen .

properties

Antiestrogens are primarily used in the treatment of breast cancer . Some tumors form a resistance of against individual antiestrogens. A distinction is made between three different antiestrogenic substance classes:

Pure antiestrogens such as fulvestrant ( Faslodex and others) act competitively as estrogen receptor antagonists.
Selective estrogen receptor modulators such as tamoxifen ( Nolvadex and others) work in the same way, but have a partially agonistic active component.
The third group, aromatase inhibitors such as anastrozole ( Arimidex et al.), Reduce the amount of oestrogens circulating in the body one metabolic step earlier by preventing the conversion of androgens into oestrogens by the aromatase enzyme .

Antiandrogens are defined analogously to antiestrogens .

literature

KE Shearer, EL Rickert, AC Peterson, RV Weatherman: Dissecting rapid estrogen signaling with conjugates. In: Steroids. Volume 77, Number 10, August 2012, pp. 968-973, doi : 10.1016 / j.steroids.2012.02.021 . PMID 22417626 . PMC 3382051 (free full text).
JM Renoir: Estradiol receptors in breast cancer cells: associated co-factors as targets for new therapeutic approaches. In: Steroids. Volume 77, Number 12, October 2012, pp. 1249-1261, doi : 10.1016 / j.steroids.2012.07.019 . PMID 22917634 .

Web links

National Cancer Institute: NCI Dictionary of Cancer Terms: Antiestrogens . Retrieved November 2, 2014.

Individual evidence

↑ A. Paradiso, S. Formenti: Hereditary breast cancer: clinical features and risk reduction strategies. In: Annals of Oncology . Volume 22 Suppl 1, January 2011, pp. I31-i36, doi : 10.1093 / annonc / mdq663 . PMID 21285148 .
↑ KL Cook, PA Clarke, R. Clarke: Targeting GRP78 and antiestrogen resistance in breast cancer. In: Future Medicinal Chemistry . Volume 5, Number 9, June 2013, pp. 1047-1057, doi : 10.4155 / fmc.13.77 . PMID 23734687 .
^ S. Roth, S. Schaad, V. Hardel, U. Jaehde: Fulvestrant . In: German Medical Weekly . 131, 2006, pp. 2718-2721.

[1] A. Paradiso, S. Formenti: Hereditary breast cancer: clinical features and risk reduction strategies. In: Annals of Oncology . Volume 22 Suppl 1, January 2011, pp. I31-i36, doi : 10.1093 / annonc / mdq663 . PMID 21285148 .

[2] KL Cook, PA Clarke, R. Clarke: Targeting GRP78 and antiestrogen resistance in breast cancer. In: Future Medicinal Chemistry . Volume 5, Number 9, June 2013, pp. 1047-1057, doi : 10.4155 / fmc.13.77 . PMID 23734687 .

[Roth-3] S. Roth, S. Schaad, V. Hardel, U. Jaehde: Fulvestrant . In: German Medical Weekly . 131, 2006, pp. 2718-2721.