Small molecule
PubChem CID 2733526
Tamoxifen
Nolvadex
- Mechanism of action
- Selective estrogen receptor modulator (SERM)
- In plain language
- Blocks estrogen from binding to its receptor in breast tissue, cutting off a signal that certain breast cancers need to grow.
- How it works
- Tamoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) that competitively binds estrogen receptors in target tissues, most notably breast tissue, preventing estradiol from exerting its proliferative effects on estrogen receptor-positive tumor cells. Its action is tissue-selective: it behaves as an estrogen antagonist in breast tissue while exhibiting partial estrogen-agonist activity in the endometrium and on bone mineral density. It is extensively metabolized hepatically to active metabolites, including endoxifen, which contribute significantly to its overall antiestrogenic potency.
- Therapeutic applications
- Indicated for treatment of metastatic breast cancer in women and men; adjuvant treatment of node-positive and node-negative breast cancer following surgery; reduction of invasive breast cancer risk in women with ductal carcinoma in situ after surgery and radiation; and reduction of breast cancer incidence in women at high risk.
- Class
- Small molecule
- Therapeutic area
- Oncology
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