Template:Tissue-specific estrogenic and antiestrogenic activity of SERMs
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Medication | Breast | Bone | Liver | Uterus | Vagina | Brain | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Lipids | Coagulation | SHBG | IGF-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
- ↑ Nath, A.; Sitruk-Ware, R. (2009). "Pharmacology and clinical applications of selective estrogen receptor modulators". Climacteric. 12 (3): 188–205. doi:10.1080/13697130802657896. ISSN 1369-7137.
- ↑ 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.
- ↑ Ellis AJ, Hendrick VM, Williams R, Komm BS (June 2015). "Selective estrogen receptor modulators in clinical practice: a safety overview". Expert Opin Drug Saf. 14 (6): 921–34. doi:10.1517/14740338.2015.1014799. PMID 25936229.
- ↑ Barbara L. Hoffman; John O Schorge; Karen D Bradshaw; Lisa M. Halvorson, Joseph I. Schaffer, Marlene M. Corton (22 April 2016). Williams Gynecology, Third Edition. McGraw-Hill Education. p. 364. ISBN 978-0-07-184909-8.
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: CS1 maint: multiple names: authors list (link) - ↑ Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". Endocrine. 54 (2): 306–314. doi:10.1007/s12020-016-1118-z. PMID 27704479.
- ↑ Baker VL, Jaffe RB (January 1996). "Clinical uses of antiestrogens". Obstet Gynecol Surv. 51 (1): 45–59. PMID 8657397.
- ↑ Bryant, Henry U. (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: 251–8. doi:10.1111/j.1749-6632.2001.tb04029.x. PMID 11795360.
- ↑ Palacios S (March 2007). "The future of the new selective estrogen receptor modulators". Menopause Int. 13 (1): 27–34. doi:10.1258/175404507780456791. PMID 17448265.
- ↑ 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.
- ↑ 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.
- ↑ McKeand WE, Orczyk GP, Ermer JC, Chines AA (July 2014). "A double-blind, randomized, ascending, multiple-dose study of bazedoxifene in healthy postmenopausal women". Clin Pharmacol Drug Dev. 3 (4): 262–9. doi:10.1002/cpdd.102. PMID 27128831.
- ↑ Trost, Landon W.; Khera, Mohit (2014). "Alternative Treatment Modalities for the Hypogonadal Patient". Current Urology Reports. 15 (7). doi:10.1007/s11934-014-0417-2. ISSN 1527-2737.