Which drug is SERM and approved by FDA for breast carcinoma with ER positive.
a. Selective estrogen receptor modulators, commonly referred to as SERMS, are a class of compounds that interact with subsets of estrogen receptors alpha and beta. SERMS are different from normal human estrogen because they bind to some tissues, repel others and display neutral activity in other tissue types.
- Based on their ability to distinguish among different estrogen receptors in the body, SERMS are being studied for use in the prevention and treatment of a number of diseases, including cancer.
- The use of SERMS in cancer is particularly aimed at hormone-dependent cancers and some breast cancers.
- The SERMS work as antagonists in this setting, by occupying receptors and making them unavailable for stimulation by human estrogen.
- Tamoxifen, also known as Nolvadex, is the oldest SERM in continuous use in the clinic. Its anti-estrogen activity was first discovered in 1962 and it was first evaluated as a contraceptive.
- Minor side effects of tamoxifen include menopausal symptoms such as hot flashes, irregular periods, vaginal irritation, headaches and fatigue. More serious side effects include increased risks of endometrial cancer, uterine sarcoma, venous thrombosis, pulmonary embolism and cataracts.
- These side effects complicate the use of tamoxifen in prevention. Although tamoxifen has been demonstrated to reduce breast cancer risk by 49 percent in high-risk women, fewer than 20 percent of these women take it as a preventive agent due to its side effects.
- Raloxifene, also known as Evista, for the reduction of invasive breast cancer among women with either osteoporosis or women considered to be at high risk for invasive breast cancer.
- Arzoxifene, another SERM, showed anti-estrogenic activity and a blocking of tumor growth in laboratory studies, The FDA has not yet approved this drug for use.