Drug intelligence / Profile preview

ICI-164384

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intramuscular
01

Overview

ICI-164384 is a steroidal antiestrogen and synthetic derivative of estradiol. It acts as a pure estrogen receptor antagonist (antiestrogen) with no intrinsic estrogenic activity. Unlike selective estrogen receptor modulators (SERMs) such as tamoxifen, it does not display partial agonist effects. Its mechanism involves binding to the estrogen receptor and inhibiting its dimerization and DNA binding ability, leading to reduced cellular content of the receptor by decreasing its half-life. The compound was developed for potential use in breast cancer treatment but was never marketed; development was discontinued in favor of fulvestrant due to higher potency[1][3][5][6][7].

Other names
N-n-butyl-N-methyl-11-(3,17β-dihydroxyestra-1,3,5(10)-trien-7α-yl)undecanamide
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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