SERMs – their role in menopause management

Key Points

  • SERMS are selective oestrogen receptor modulators - chemicals that have differing agonist or antagonist effects at the oestrogen receptor in different tissues
  • different SERMS have different clinical applications, such as ovulation induction, treatment of osteoporosis, reduction in breast cancer risk or recurrence, treatment of vaginal atrophy and dyspareunia
  • not all SERMS are available in all countries

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SERMs is “shorthand” for a class of drug called selective oestrogen receptor modulators. They are a versatile group of drugs that can be used to treat/ prevent several conditions such as osteoporosis, infertility and hormone responsive cancers. Within the SERM class, different compounds have differing agonist or antagonist effects at the oestrogen receptor in different tissues, therefore they are “selective” (1, 2).

Newer SERMs are being developed with more favourable oestrogen receptor selectivity i.e. utilising the positive effects of oestrogen, such as preventing osteoporosis and treating genital atrophy (vaginal dryness), without stimulating breast cancer cells or inducing endometrial hyperplasia. These agents aim to minimise the negative effects of the older agents.

Different kinds of SERMS

Naturally occurring SERMs include plant-derived oestrogens or phyto-oestrogens that are sometimes used to treat symptoms of menopause. (see AMS Information Sheet Complementary and Herbal Therapies for Hot Flushes).

Clomiphene citrate is an early SERM which is used to induce ovulation in women desiring pregnancy because it acts as an oestrogen antagonist at the pituitary and increases gonadotrophin drive to the ovary.

Tamoxifen

Raloxifene

Bazedoxifene          

Ospemifene

Lasofoxifene

References

1. Anthony M, Williams JK, Dunn BK. What would be the properties of an ideal SERM? Ann N Y Acad Sci. 2001;949:261-78.

2. Pickar JH, Mirkin S. Tissue-selective agents: selective estrogen receptor modulators and the tissue-selective estrogen complex. Menopause International. 2010;16(3):121-8.

3. Hitisha K Patel, Teeru Bihani. Pharmacol Ther. 2018 Jun;186:1-24.

Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment

4. Mirkin S, Komm BS. Tissue-selective estrogen complexes for postmenopausal women. Maturitas. 2013;76(3):213-20.

5. Gizzo S, Saccardi C, Patrelli TS, Berretta R, Capobianco G, Di Gangi S, et al. Update on raloxifene: mechanism of action, clinical efficacy, adverse effects, and contraindications. Obstet Gynecol Surv. 2013;68(6):467-81.

6. Pinkerton JV, Harvey JA, Lindsay R, Pan K, Chines AA, Mirkin S, et al. Effects of bazedoxifene/conjugated estrogens on the endometrium and bone: a randomized trial. J Clin Endocrinol Metab. 2014;99(2):E189-198.

7. Archer DF, Carr BR, Pinkerton JV, Taylor HS, Constantine GD. Effects of ospemifene on the female reproductive and urinary tracts: translation from preclinical models into clinical evidence. Menopause. 2015;22(7):786-96.

8. Muriel Laine et al Breast Cancer Res. 2021 May 12;23(1):54. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer

AMS Empowering Menopausal Women

Note: 

Medical and scientific information provided and endorsed by the Australasian Menopause Society might not be relevant to a particular person's circumstances and should always be discussed with that person's own healthcare provider. This Information Sheet contains copyright or otherwise protected material. Reproduction of this Information Sheet by Australasian Menopause Society Members and other health professionals for clinical practice is permissible. No other reproduction or transmission is permitted in any form or by any information storage and retrieval systems except as permitted under the Copyright Act 1968 or with prior written permission from the copyright owner. ID:2023-05-16 

Content updated May 2023

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