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Importance of Selective Estrogen Receptor Modulators as Potential Multiple Therapeutic Agents

Abstract

Selective estrogen receptor modulators (SERMs) are a group of drugs with diverse structural chemical characteristics that are characterized as high-affinity ligandsto estrogenic receptors (ERs) but have the peculiarity of triggering estrogen-agonist or estrogen-antagonist actions, depending on the tissue in which they act. From a pharmacological perspective, SERMs should be segregated from pure antiestrogens, such as fulvestrant. Which are molecules chemically related to estradiol and exclusively exhibit estrogenic antagonist activity. SERMs also should be distinguished from the so-called “gonad mimetic” drugs, such as tibolone, that act by means of non-selective binding to different types of sex steroid receptors. A number of novel groups of synthetic compounds called Selective Estrogen Receptor Modulators (SERMs) have been discovered and are currently in use or under various stages of clinical evaluation, while several new compounds continue to appear in the patent literature. Although published clinical trial data are limited, these novel compounds are being evaluated for the prevention and treatment of hormone-responsive cancer, for prevention and treatment of post-menopausal osteoporosis and for prevention of cardiovascular disease and other estrogen deficiency-related indications.

Avidha K, Ruchi B, Nidhi S, Richa K* and Jaya P*

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