Selective estrogen receptor modulators: an update on recent clinical findings

Shelly, Wendy; Draper, Michael W.; Krishnan, Venkatesh; Wong, Mayme; Jaffe, Robert B.

doi:10.1097/ogx.0b013e31816400d7

Cited by 193Estrogen and related hormone effectsBreast Cancer Treatment StudiesAdvanced Breast Cancer Therapies

Selective estrogen receptor modulators: an update on recent clinical findings

Shelly, Wendy, Draper, Michael W., Krishnan, Venkatesh, Wong, Mayme, Jaffe, Robert B.·2008·Obstetrical & Gynecological Survey

DOI 10.1097/ogx.0b013e31816400d7

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Abstract

Recent clinical data on selective estrogen receptor modulators (SERMs) have provided the basis for reassessment of the SERM concept. The molecular basis of SERM activity involves binding of the ligand SERM to the estrogen receptor (ER), causing conformational changes which facilitate interactions with coactivator or corepressor proteins, and subsequently initiate or suppress transcription of target genes. SERM activity is intrinsic to each ER ligand, which accomplishes its unique profile by specific interactions in the target cell, leading to tissue selective actions. We discuss the estrogenic and anti-estrogenic effects of early SERMs, such as clomiphene citrate, used for treatment of ovulation induction, and the triphenylethylene, tamoxifen, which has ER antagonist activity in the breast, and is used for prevention and treatment of ER-positive breast cancer. Since the development of tamoxifen, other triphenylethylene SERMs have been studied for breast cancer prevention, including droloxifene, idoxifene, toremifene, and ospemifene. Other SERMs have entered clinical development more recently, including benzothiophenes (raloxifene and arzoxifene), benzopyrans (ormeloxifene, levormeloxifene, and EM-800), lasofoxifene, pipendoxifene, bazedoxifene, HMR-3339, and fulvestrant, an anti-estrogen which is approved for breast cancer treatment. SERMs have effects on tissues containing ER, such as the breast, bone, uterine and genitourinary tissues, and brain, and on markers of cardiovascular risk. Current evidence indicates that each SERM has a unique array of clinical activities. Differences in the patterns of action of SERMs suggest that each clinical end point must be evaluated individually, and conclusions about any particular SERM can only be established through appropriate clinical trials. Target Audience: Obstetricians & Gynecologists, Family Physicians Learning Objectives: After completion of this article, the reader should be able to summarize the complex function and interactions of selective estrogen receptor modulators (SERMs); recall their suppression or initiation of target genes leading them to their actions; and explain their important roles in breast cancer treatment and possible side effects on bone, the genitourinary system, and on markers of cardiovascular risk.

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Clomiphene citrate is a selective oestrogen receptor modulator with both oestrogenic and antioestrogenic properties.
“Clomiphene citrate is a selective oestrogen receptor modulator with both oestrogenic and antioestrogenic properties. 216”
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Estrogen actions in the brain and the basis for differential action in men and women: a case for sex-specific medicines
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Authors: Shelly, W., Draper, M. W., Krishnan, V., Wong, M., & Jaffe, R. B.
Affiliations: University of California, San Francisco (US)
Eli Lilly (United States) (US)
Corresponding author: Shelly, Wendy
ORCID: Krishnan, Venkatesh
Venue: Obstetrical & Gynecological Survey
Publisher: Ovid Technologies (Wolters Kluwer Health)
Published: 2008-03
Volume: 63
Issue: 3
Pages: 163-181
ISSN: 0029-7828 (ISSN-L)
DOI: 10.1097/ogx.0b013e31816400d7
OpenAlex: W201704258
Cited by: 193
References: 186
Citations by year: 2026: 1 · 2025: 7 · 2024: 6 · 2023: 4 · 2022: 6 · 2021: 4 · 2020: 6 · 2019: 11 · 2018: 9 · 2017: 4 · 2016: 9 · 2015: 8 · 2014: 13 · 2013: 16 · 2012: 16
FWCI: 2.30
Type: journal article
Language: en
Open access: closed
Locations: Obstetrical & Gynecological Survey (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
Keywords: selective estrogen receptor modulators, estrogen receptor, tamoxifen, clomiphene citrate, breast cancer, breast cancer prevention, fulvestrant, raloxifene, aromatase inhibitors, bone effects, cardiovascular risk
MeSH terms: Breast Neoplasms, Female, Gene Expression Regulation, Humans, Ovulation Induction, Receptors, Estrogen, Urogenital System, Bone Density, Postmenopause, Selective Estrogen Receptor Modulators

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Selective estrogen receptor modulators: an update on recent clinical findings

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