Selective Estrogen Receptor Modulators: Clinical Spectrum*

Selective Estrogen Receptor Modulators

Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive differ...

Selective estrogen receptor modulators (SERMS).

Hormone receptors and, specifically, estrogen receptors were described about four decades ago. For estrogens, there are two receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). The two receptors are coded by different genes and their tissue expression varies across organs. ERalpha is predominantly expressed in reproductive tissues (uterus, breast, ovaries) liver and...

Selective estrogen receptor modulators: tissue specificity and clinical utility

Selective estrogen receptor modulators (SERMs) are a diverse group of nonsteroidal compounds that function as agonists or antagonists for estrogen receptors (ERs) in a target gene-specific and tissue-specific fashion. SERM specificity involves tissue-specific expression of ER subtypes, differential expression of co-regulatory proteins in various tissues, and varying ER conformational changes in...

Selective estrogen receptor modulators and cardiovascular events.

ost of the previous observational studies suggest that estrogen replacement therapy reduces cardiovascular risks,1 but meta-analysis of randomized clinical trials showed increased risk of hormone replacement therapy for cardiovascular events.2 Both hypercoagulability and upregulation of inflammation-sensitive proteins could underline the increased risk of estrogen treatment in coronary artery d...

Screening Assay for Selective Estrogen Receptor Modulators