Tamoxifen

Synthetic. Chemical. CAS: 10540-29-1. Formula: C26H29NO. MW: 371.51. Synthetic. Selective estrogen receptor modulator (SERM) used as adjuvant therapy for estrogen-dependent breast cancer. Antagonist of ER action in breast tissue and breast cancer cells and ER agonist in bone, uterus, and the cardiovasculature system. This prodrug is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen) and 4-hydroxy-TMX (afimoxifene). N,N-Didesmethyl-4-hydroxytamoxifen (norendoxifen), another active metabolite has been found to act as a potent competitive aromatase inhibitor and may also be involved in its antiestrogenic activity. Binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy. Protein kinase C (PKC) inhibitor and anti-angiogenetic factor.