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4'-fluorodesmethylarzoxifen
- Development stage
- Preclinical
- Lead developer
- University of Illinois Chicago
- Modality
- Small Molecules
- Administration
- Subcutaneous
01
Overview
4'F-DMA (4'-fluorodesmethylarzoxifen) is a preclinical selective estrogen receptor modulator (SERM) developed by the University of Illinois at Chicago. It is a fluorinated derivative of desmethylarzoxifene (DMA), which is the active metabolite of the benzothiophene SERM arzoxifene. 4'F-DMA was designed to improve metabolic stability and reduce toxicity compared to DMA and raloxifene. Specifically, the 4'-fluoro substitution prevents the oxidative bioactivation of the compound into electrophilic and potentially genotoxic diquinone methides (quinoids), which can cause glutathione depletion and DNA damage. 4'F-DMA binds to both estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ), exhibiting antiestrogenic activity comparable to raloxifene in breast cancer and endometrial cell lines without displaying estrogenic properties.
- Other names
- 4'-fluoro-desmethylarzoxifenfluoro-substituted desmethyl arzoxifene
02
Targets
ESR2 (ERβ)ESR1 (ERα)
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