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Cited by 205Estrogen and related hormone effectsMenopause: Health Impacts and TreatmentsPhytoestrogen effects and research

A pharmacological review of selective oestrogen receptor modulators

Goldstein, S. R.·2000·Human Reproduction Update
DOI 10.1093/humupd/6.3.212
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Abstract

Selective oestrogen receptor modulators (SERMs) are structurally diverse non-steroidal compounds that bind to oestrogen receptors and produce oestrogen agonist effects in some tissues and oestrogen antagonist effects in others. SERMs are being evaluated for a number of oestrogen-related diseases, including post-menopausal osteoporosis, hormone-dependent cancers, and cardiovascular disease. Several compounds that exhibit a SERM profile are currently available for clinical use, including clomiphene, tamoxifen, and toremifene (which are triphenylethylenes) and raloxifene (a benzothiophene). Clomiphene is used for the induction of ovulation in sub-fertile women attempting pregnancy. Tamoxifen and toremifene are both used to treat breast cancer. Tamoxifen may have beneficial effects on bone mineral density and serum lipids. The effects of toremifene on serum lipids are similar to that of tamoxifen. Both compounds have stimulatory effects on the endometrium. Raloxifene, indicated for the treatment and prevention of post-menopausal osteoporosis, has beneficial effects on bone mineral density and serum lipids, but does not increase the risk of endometrial hyperplasia or endometrial cancer. Recently, raloxifene was shown to reduce the incidence of vertebral fractures in otherwise healthy women with osteoporosis; in the same study, a reduced incidence of breast cancer was also observed. Similar to oestrogens, SERMs increase the incidence of venous thromboembolism. Several newer compounds that exhibit a SERM profile are also in clinical development, including other triphenylethylenes (droloxifene, idoxifene) and benzothiophenes (LY353381.HCl), benzopyrans (EM-800), and naphthalenes (CP-336,156).

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Crossref · 10.1093/humupd/6.3.212

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  • The tamoxifen-inducible Global-ARKO data must be interpreted with caution because AR gene knockdown is not complete (approximately 20% mRNA expression remained) and tamoxifen induction may affect fat mass through ER signaling.

    “These data, however, must be interpreted with some caution as AR gene knockdown is not complete (approximately 20% mRNA expression remained) and the induction of knockdown via tamoxifen, despite the short induction time (4 days), may pose some effect of fat mass through ER signaling.”

    From The role of the androgen receptor in the pathogenesis of obesity and its utility as a target for obesity treatments (2022) · cites this paper as [149]

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Authors
Goldstein, S. R.
Affiliations
NYU Langone Health (US)
Corresponding author
Goldstein, S. R.
ORCID
Goldstein, S. R.
Venue
Human Reproduction Update
Publisher
Oxford University Press (OUP)
Published
2000-05-01
Volume
6
Issue
3
Pages
212-224
ISSN
  • 1355-4786 (ISSN-L)
  • 1460-2369
DOI
10.1093/humupd/6.3.212
OpenAlex
W2131184855
Cited by
205
References
123
Citations by year
2026: 7 · 2025: 4 · 2024: 7 · 2023: 5 · 2022: 16 · 2021: 9 · 2020: 12 · 2019: 2 · 2018: 4 · 2017: 6 · 2016: 7 · 2015: 11 · 2014: 13 · 2013: 11 · 2012: 7
FWCI
3.69
Type
journal article
Language
en
Open access
closed
Locations
  • Human Reproduction Update (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Eli Lilly and Company
  • National Cancer Institute
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
  • Health Sciences › Medicine › Pathology and Forensic Medicine › Phytoestrogen effects and research
Keywords
selective estrogen receptor modulators, oestrogen receptor, clomiphene citrate, tamoxifen, toremifene, raloxifene, breast cancer, cardiovascular disease, bone mineral density, serum lipids, endometrial hyperplasia, venous thromboembolism, droloxifene, idoxifene, triphenylethylene, benzothiophene, benzopyrans, naphthalene
MeSH terms
Breast Neoplasms, Clomiphene, Female, Humans, Ovulation Induction, Tamoxifen, Osteoporosis, Postmenopausal, Toremifene, Selective Estrogen Receptor Modulators, Raloxifene Hydrochloride

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