Selective estrogen receptor modulators (SERMs) are estrogen receptor (ER) ligands that exhibit either estrogen agonistic or antagonistic activity in a tissue-specific manner. The first and second generation SERMs, tamoxifen and raloxifene, are used for treatment of ER positive breast cancer and postmenopausal osteoporosis respectively. The third-generation SERM, bazedoxifene (BZA), effectively prevents osteoporosis while blocking the estrogenic stimulation in breast and uterus. Notably, BZA combined with conjugated estrogens (CE) in a tissue-selective estrogen complex (TSEC) is a new menopausal treatment. Postmenopausal estrogen deficiency predisposes to metabolic syndrome and type 2 diabetes, and therefore the effects of SERMs and TSECs on metabolic homeostasis are gaining attention. In this article, we summarize current knowledge about the impact of SERMs on metabolic homeostasis and metabolic disorders in animal models and postmenopausal women.
Bibliographical noteFunding Information:
FMJ received research funding from Pfizer, Inc. Other authors declare no competing financial interest.
We apologize to those investigators and studies we were unable to cite in this Review because of space limitation. We thank Loula Burton at Tulane University Health Sciences Center for editorial assistance. This work was supported by grants from the National Institutes of Health ( DK074970 , HD044405 ), the American Diabetes Association ( 7-13-BS-101 ) and an investigator initiated grant from Pfizer, Inc to F.M.J.
© 2015 Published by Elsevier B.V.
- Energy metabolism
- Metabolic syndrome
- Selective estrogen receptor modulators
- Tissue-selective estrogen complex