Acta Scientific Women's Health (ASWH)

Receptors Modulators (SERM)-a Narrative Minireview Volume 6 Issue 7

An Update on Therapy for Postmenopausal Symptoms with Emphasis on Selective Estrogen Receptors Modulators (SERM)-a Narrative Minireview

Kulvinder Kochar Kaur*

M.D Obstetrics and Gynaecology, specialist Reproductive Endocrinology and Infertility Specialist, Punjab, India

*Corresponding Author: Kulvinder Kochar Kaur, M.D Obstetrics and Gynaecology, specialist Reproductive Endocrinology and Infertility Specialist, Punjab, India.

Received: April 12, 2024; Published: June 21, 2024

Abstract

Treatment for problematic menopausal vasomotor symptoms as hormonal replacement’ therapy has been debatable. Estrogen portrays a critical controlling hormone in the working the female reproductive system. Estrogen hormone controls a plethora of complicated physiological events. Possessing apart in reproduction, skeletal as well as cardiovascular system through actions on the two kinds of estrogen receptors-- estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) which portray unresearched transcription factors. Selective estrogen receptors modulators (SERM)are presently utilized for the treatment of bone elimination, breast cancer in addition to menopausal symptoms, metabolic along with neurodegenerative diseases; their properties which aids in their working in the form of agonist along with antagonist based on the target tissues. Tamoxifen: the first generation SERM utilization is in the form of adjuvant for the breast cancer having lesser risk in the premenstrual females as well as avoidance of breast cancer that is ER positive. Raloxifene: a second generation SERM portrays a significant for the treatment as well as avoidance of osteoporotic fractures in post menopausal women with avoidance of compression fractures of vertebral column. Innovative SERM molecules have become accessible, have corroborated they possess greater efficacy for the treatment of as well as avoidance of osteoporosis. They are inclusive of lasofoxifene, bazedoxifene, arzoxifene, along with ospemifene. Advantages of raloxifene vs bazedoxifene are getting evaluated. Although they possess therapeutic advantages and effects they do possess displayed inimical sequelae like venous thromboembolism (VTE). escalated endometrial cancer risk has been correlated with tamoxifen. Here we describe generation, invention and newer SERM’s like lasofoxifene, bazedoxifene, arzoxifene, and ospemifene. Bazedoxifene might be used to avoid DM in menopausal ladies.

Keywords: menopausal symptoms; hormonal replacement’ therapy; Selective estrogen receptors modulators (SERM)

References

  1. Genazzani AR., et al. “Hormone therapy in the post menopausalyears: considering benefits and risks in clinical practice”. Human Reproduction Update 27 (2021): 1115-1150.
  2. Burger HG. “Selective estrogen receptors modulators”. Hormone Biology 3 (2019): 25-29.
  3. Bryant HU. “Selective estrogen receptors modulators”. Reviews in Endocrine and Metabolic Disorders 3 (2002): 221-41.
  4. Yasul T., et al. “Biological effects of hormonal replacement’ therapy in relation to serumestradiol levels”. Hormone Research 56 (2001): 38-44.
  5. Andrews WC. “Continuous combined estrogen/progestin hormonal replacement’ therapy”. Clinical Therapeutics 17 (1995): 812-826.
  6. Kapoor E., et al. “Menopausal hormonal therapy in women with conditions”. Best Practice and Research Clinical Obstetrics and Gynaecology 35 (2021):
  7. Pollock JA and Parker HK. “Advances in the development of prodrugs as selective modulators of estrogen receptors”. Journal of the Endocrine Society 6 (2022):
  8. Katzenllenbogen BS and Katzenllenbogen JA. “Estrogen receptors transcription and transactivation: estrogen receptor alpha and estrogen receptor beta: regulation of selective estrogen receptors modulators and importance in breast cancer”. Breast Cancer Research 2 (2000): 335-344.
  9. Dowers TS., et al. “Bioactivation of selective estrogen receptors modulators (SERM)”. Chemical Research in Toxicology 19 (2006): 1125-1137.
  10. Martinkovich S., et al. “Selective estrogen receptors modulators: tissue specificity and clinical utility”. Clinical Interventions in Aging 9 (2014): 1437-1452.
  11. Grese TA., et al. “Molecular determinants of tissue selectivity in estrogen receptors modulators”. Proceedings of the National Academy of Sciences of the United States of America 94 (1997): 14105-14110.
  12. An KC. “Selective estrogen receptors modulators”. Asian Spine Journal 10 (2016): 787-791.
  13. , et al. “Update on hormonal therapy for the of post menopausal women”. BioScience Trends (2022): 46-57.
  14. , et al. “Updates on therapeutic alternatives of genitourinary syndrome of menopause: hormonal and nonhormonal management”. Journal of Menopausal Medicine 27 (2021): 1-7.
  15. Carrol DG and Noble SL. “Hormonal replacement’ therapy: current concerns and considerations”. The American Journal of Managed Care 8 (2002): 663-675.
  16. Naumova I and Castelo Branco C. “Current treatment options for post menopausal vaginal atrophy”. International Journal of Women's Health 10 (2018): 387-395.
  17. , et al. “Vaginal health in menopausal women”. Medicina (Kaunas) 55 (2019): 615.
  18. Edwards D and Panay N. “Treating vulvovaginal atrophy/genitourinary syndrome of menopause: how important is vaginal lubricants and moisturized composition?” Climacteric 19 (2016): 151 -61.
  19. Gambacciani M. “Selective estrogen receptors modulators in menopause”. Minerva Ginecologica 65 (2013): 621-630.
  20. Mehta J., et al. “Risks, benefits and treatment modalities of menopausal hormonal therapy: Current concepts”. Frontiers in Endocrinology (Lausanne) 12 (2021):
  21. Sanchez-Borrego., et al. “Efficacy and safetyof a phyto SERM as an alternative to hormone therapy”. Climacteric 18 (2015): 350-357.
  22. Maximov PY., et al. “The discovery and development of selective estrogen receptors modulators (SERM) for clinicalpractice”. Current Clinical Pharmacology 8 (2013): 135-155.
  23. Motlami G., et al. “Novel advances in the role of Selective estrogen receptors modulators in hormonal replacement’ therapy:a paradigm shift”. Cureus11 (2023): e49079.
  24. Howell A and Howell SJ. “Tamoxifen evolution”. British Journal of Cancer 128 (2023): 421-430.
  25. Scott JA., et al. “Raloxifene:a Selective estrogen receptors modulator”. American Family Physician 60 (1999): 1131-1139.
  26. Letha by A., et al. “Hormonal replacement’ therapy for cognitive function in post menopausal women”. Cochrane Database of Systematic Reviews 2008 (2008):
  27. Gennari L., et al. “Selective estrogen receptors modulators for post-menopausal, osteoporosis”. Drugs Ageing 24 (2007): 361-379.
  28. Mitwally MF. “Bazedoxifene: a selective estrogen receptors modulator”. Womens Health (London) 4 (2008): 319-326.
  29. Cummings SR., et al. “Arzoxifene for prevention of fractures and invasive breast cancer”. Journal of Bone and Mineral Research 26 (2011): 397-404.
  30. De Gregario MW., et al. “Ospemifene:a first in class non selective estrogen receptors modulator approved for the treatment of dyspareunia associated with vulvar and vaginal atrophy”. Steroids 90 (2014): 82-93.
  31. , et al. “The effect of selective estrogen receptors modulators on type2 diabetes onset in women: basic and clinical insights”. Journal of Diabetes and its Complications 31 (2017): 773-779.
  32. Pan M., et al. “Drugs for the treatment of postmenopausal symptoms: Hormonal and non-hormonal therapy”. Life Sciences 312 (2023): 121
  33. Mikus M., et al. “Pharmacokinetics and safety of the available medical options in the treatment of endometriosis”. Pharmaceuticals 16 (2023):
  34. Matsushima-Nishikawi R., et al. “SERMs (selective estrogen receptor modulator), acting as estrogen receptor β agonists in hepatocellular carcinoma cells, inhibit the transforming growth factor-α-induced migration via specific inhibition of AKT signaling pathway”. PLOS One 17 (2022):
  35. Kulvinder Kochar Kaur., et al. “Pharmacologic non Pharmacologic management of fractures risk for optimizing fractures prevention in potential osteoporotic women (post-menopausal and peri menopausal) women- a systematic review”. Iatrology Archives2 (2020): 1-12.

Citation

Citation: Kulvinder Kochar Kaur. “An Update on Therapy for Postmenopausal Symptoms with Emphasis on Selective Estrogen Receptors Modulators (SERM)-a Narrative Minireview".Acta Scientific Women's Health 6.7 (2024): 05-12.

Copyright

Copyright: © 2024 Kulvinder Kochar Kaur. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.




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