Abstract
Oestrogen is the key regulatory hormone for the development and maintenance of reproductive functions and affects various physiological systems, including the skeletal, cardiovascular, and central nervous systems. oestrogen replacement therapy (ERT) is highly effective in postmenopausal women, addressing menopausal symptoms and providing beneficial effects on osteoporosis and coronary heart disease. However, ERT is associated with significant side effects, such as an increased risk of breast cancer. To mitigate these risks, selective oestrogen receptor modulators (SERMs) have been developed. SERMs are a growing class of synthetic nonsteroidal compounds that act as oestrogen receptor agonists or antagonists in a tissue-specific manner. They can selectively activate or inhibit oestrogen receptors in different tissues throughout the body. SERMs are used to treat a variety of conditions, including ER-positive breast cancer, osteoporosis, coronary heart disease, Alzheimer’s disease, and cholesterol metabolism disorders in postmenopausal women. Specific SERMs are employed for different conditions: raloxifene for osteoporosis, tamoxifen and toremifene for breast cancer, clomiphene for the induction of ovulation, and ormeloxifene for oral contraception. Arzoxifene is used for altering cholesterol metabolism. Each SERM forms a unique complex with oestrogen receptors, influencing target tissues and resulting in a tissue-selective pharmacological profile. This unique mechanism of action translates into specific safety and efficacy profiles for each SERM. The surprising pharmacology of SERMs has sparked interest in developing new selective medications, allowing for precise treatment of various diseases. This article reviews the pharmacological properties of SERMs and explains how they differ from oestrogen in their actions.
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