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Usage

Uses

Used in Pharmaceutical Industry:
Endoxifen HCl is used as a breast cancer treatment for patients who do not respond well to tamoxifen due to its more potent estrogen receptor binding and anti-estrogenic properties.
Endoxifen HCl is used as a preventive measure for the development of breast cancer in high-risk individuals, as research suggests its potential effectiveness in reducing the risk of breast cancer.
Endoxifen HCl is used in ongoing clinical research to determine its safety and efficacy in various breast cancer treatment settings, with the aim of providing a more effective alternative to tamoxifen for patients who do not respond well to the current standard of care.

Upstream product

• 1231730-32-7 (4-hydroxyphenyl)(4-(2-(methylamino)ethoxy)phenyl)methanone hydrochloride 
• 93-55-0 1-phenyl-propan-1-one 

Relevant academic research and scientific papers

A convenient synthesis of (Z)-4-hydroxy-N-desmethyltamoxifen (endoxifen)

A mixture of the (Z)- and (E)-isomers of 4-hydroxy-N-desmethyltamoxifen was conveniently prepared in four steps. These geometrical isomers were then neatly separated by semi-preparative Reverse Phase High Performance Liquid Chromatography (RP-HPLC) using specified conditions. Additionally, the isolated E-isomer could be equilibrated in aqueous strong acid in acetonitrile or trifluoroacetic acid/dichloromethane to give a clean 1:1 mixture of Z/E isomers that was re-subjected to HPLC separation. In this way, most of the undesired (E)-isomer could be readily converted to the desired (Z)-isomer providing quick access to over 200 mg quantities of pure endoxifen (Z-isomer), a potent antiestrogenic metabolite of tamoxifen traditionally used in breast cancer treatment.