Fulvestrant: An Estrogen Receptors Antagonist with a Unique Structure and Mode of Action
Many breast cancers have estrogen receptors (ERs) and the growth of these tumors can be stimulated by estrogen. ER antagonists bind to ER and downregulate the ER protein in breast cancer cells. Fulvestrant (ICI 182,780) is an ER antagonist with a unique structure and mode of action. It not only binds competitively to the ER with high affinity, but also acts as a degradation inducer of ER with its long alkyl side chain. Therefore, fulvestrant has been reported to help circumvent resistance to “pure” ER antagonists, such as tamoxifen citrate [
T2510]. For your reference, [
D5471] is a key synthetic intermediate of fulvestrant. (The product is for research purpose only.)