CAS: 1032008-74-4

Endoxifen is a selective estrogen receptor modulator. It binds to estrogen receptors and blocks the effects of estrogen. Endoxifen has been shown to be effective for the treatment of breast cancer. The drug has a high degree of bioavailability in vivo and can be administered by mouth. It is metabolized by CYP2D6, and its plasma levels are increased when combined with CYP3A4 inhibitors or inducers. Endoxifen is used to control cancerous cell growth and prevent bone resorption in humans. This drug also inhibits cholesterol synthesis by blocking the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase).

Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.