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The molecular mechanism of action for Fulvestrant. Fulvestrant, being a pure steroidal ERα antagonist, inhibits the dimerization of the estrogen receptor and blocks the nuclear localization of the receptor itself. The binding of fulvestrant with ER also leads to a rapid degradation of the fulvestrant-ER complex and makes the receptor unavailable to estrogens, so the ability of ER to promote gene transcription is attenuated.
