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toremifene
- Development stage
- Approved
- Lead developer
- Orion Pharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Toremifene is a first-generation nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene class, structurally related to tamoxifen. It is used primarily for the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor-positive or unknown-status tumors. Toremifene acts as an estrogen antagonist on breast tissue by competitively binding to estrogen receptors, thereby blocking the growth-stimulating effects of estrogen in hormone-dependent tumors. In other tissues, it can exert partial agonist (estrogenic) effects, such as on bone and cardiovascular system. The drug may also inhibit tumor growth through induction of apoptosis and regulation of oncogene expression and growth factors[1][3][4][6]. Its only approved indication in the United States is for metastatic breast cancer in postmenopausal women[7].
- Brand names
- Fareston
- Other names
- toremifene citrate
02
Targets
ESR1 (ERα)
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