| 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] | ||||||||||||||
Template documentationUsage
This template can be used to easily insert a table detailing tissue-specific estrogenic and antiestrogenic activity of SERMs into an article. It comes with sixteen pre-provided references.
By passing the parameter |state=mw-collapsed, the table can be displayed as collapsed by default.
References
- ^ Nath A, Sitruk-Ware R (June 2009). "Pharmacology and clinical applications of selective estrogen receptor modulators". Climacteric. 12 (3): 188–205. doi: 10.1080/13697130802657896. PMID 19387883. S2CID 25111733.
- ^ 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. S2CID 23817729.
- ^ 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.
- ^ 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. S2CID 10136018.
- ^ 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.
- ^ 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. S2CID 29053109.
- ^ 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.
- ^ 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. S2CID 10163257.
- ^ Trost LW, Khera M (July 2014). "Alternative treatment modalities for the hypogonadal patient". Current Urology Reports. 15 (7): 417. doi: 10.1007/s11934-014-0417-2. PMID 24817260. S2CID 20304701.
| 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] | ||||||||||||||
Template documentationUsage
This template can be used to easily insert a table detailing tissue-specific estrogenic and antiestrogenic activity of SERMs into an article. It comes with sixteen pre-provided references.
By passing the parameter |state=mw-collapsed, the table can be displayed as collapsed by default.
References
- ^ Nath A, Sitruk-Ware R (June 2009). "Pharmacology and clinical applications of selective estrogen receptor modulators". Climacteric. 12 (3): 188–205. doi: 10.1080/13697130802657896. PMID 19387883. S2CID 25111733.
- ^ 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. S2CID 23817729.
- ^ 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.
- ^ 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. S2CID 10136018.
- ^ 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.
- ^ 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. S2CID 29053109.
- ^ 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.
- ^ 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. S2CID 10163257.
- ^ Trost LW, Khera M (July 2014). "Alternative treatment modalities for the hypogonadal patient". Current Urology Reports. 15 (7): 417. doi: 10.1007/s11934-014-0417-2. PMID 24817260. S2CID 20304701.