Template:Tissue-specific_estrogenic_and_antiestrogenic_activity_of_SERMs
Template:Tissue-specific estrogenic and antiestrogenic activity of SERMs
More information Medication, Breast ...
| Medication | Breast | Bone | Liver | Uterus | Vagina | Brain | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Lipids | Coagulation | SHBGTooltip Sex hormone-binding globulin | IGF-1Tooltip Insulin-like growth factor 1 | Hot flashes | Gonadotropins | |||||||||
| Estradiol | + | + | + | + | + | + | + | + | + | + | ||||
| "Ideal SERM" | – | + | + | ± | ± | ± | – | + | + | ± | ||||
| Bazedoxifene | – | + | + | + | + | ? | – | ± | – | ? | ||||
| Clomifene | – | + | + | ? | + | + | – | ? | – | ± | ||||
| Lasofoxifene | – | + | + | + | ? | ? | ± | ± | – | ? | ||||
| Ospemifene | – | + | + | + | + | + | ± | ± | – | ± | ||||
| Raloxifene | – | + | + | + | + | + | ± | – | – | ± | ||||
| Tamoxifen | – | + | + | + | + | + | + | – | – | ± | ||||
| Toremifene | – | + | + | + | + | + | + | – | – | ± | ||||
| Effect: + = Estrogenic / agonistic. ± = Mixed or neutral. – = Antiestrogenic / antagonistic. Note: SERMs generally increase gonadotropin levels in hypogonadal and eugonadal men as well as premenopausal women (antiestrogenic) but decrease gonadotropin levels in postmenopausal women (estrogenic). Sources: [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16] | ||||||||||||||
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References
- Morello KC, Wurz GT, DeGregorio MW (July 2002). "SERMs: current status and future trends". Crit. Rev. Oncol. Hematol. 43 (1): 63–76. doi:10.1016/S1040-8428(02)00022-7. PMID 12098608.
- Martinkovich S, Shah D, Planey SL, Arnott JA (2014). "Selective estrogen receptor modulators: tissue specificity and clinical utility". Clin Interv Aging. 9: 1437–52. doi:10.2147/CIA.S66690. PMC 4154886. PMID 25210448.
- Mirkin S, Pickar JH (January 2015). "Selective estrogen receptor modulators (SERMs): a review of clinical data". Maturitas. 80 (1): 52–7. doi:10.1016/j.maturitas.2014.10.010. PMID 25466304.
- Barbara L. Hoffman; John O. Schorge; Karen D. Bradshaw; Lisa M. Halvorson; Joseph I. Schaffer; Marlene M. Corton (22 April 2016). Williams Gynecology (Third ed.). McGraw-Hill Education. p. 364. ISBN 978-0-07-184909-8.
- Baker VL, Jaffe RB (January 1996). "Clinical uses of antiestrogens". Obstet Gynecol Surv. 51 (1): 45–59. doi:10.1097/00006254-199601000-00021. PMID 8657397.
- Bryant HU (2008). "Chapter 41 – The Pharmacology of Selective Estrogen Receptor Modulators". Principles of Bone Biology. pp. 887–919. doi:10.1016/B978-0-12-373884-4.00058-6.
- Tsourdi E, Kourtis A, Farmakiotis D, Katsikis I, Salmas M, Panidis D (April 2009). "The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia". Fertil. Steril. 91 (4 Suppl): 1427–30. doi:10.1016/j.fertnstert.2008.06.002. PMID 18692782.
- Plouffe L, Siddhanti S (December 2001). "The effect of selective estrogen receptor modulators on parameters of the hypothalamic-pituitary-gonadal axis". Ann. N. Y. Acad. Sci. 949 (1): 251–8. Bibcode:2001NYASA.949..251P. doi:10.1111/j.1749-6632.2001.tb04029.x. PMID 11795360. S2CID 27000923.
- Bondi C, Ferrero S, Scala C, Tafi E, Racca A, Venturini PL, Leone Roberti Maggiore U (October 2016). "Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause". Expert Opin Drug Metab Toxicol. 12 (10): 1233–46. doi:10.1080/17425255.2016.1218847. PMID 27476551. S2CID 9637902.
- Roelfsema F, Yang RJ, Takahashi PY, Erickson D, Bowers CY, Veldhuis JD (February 2018). "Effects of Toremifene, a Selective Estrogen Receptor Modulator, on Spontaneous and Stimulated GH Secretion, IGF-I, and IGF-Binding Proteins in Healthy Elderly Subjects". J Endocr Soc. 2 (2): 154–165. doi:10.1210/js.2017-00457. PMC 5789038. PMID 29383334.
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