Norendoxifen
Also called Z-Norendoxifen
Part of the metabolic pathway of Tamoxifen. See the timeline on the metabolic highway.
Overview
Norendoxifen, also known as 4-hydroxy-N,N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor (AI) of the triphenylethylene group that was never marketed.[1] WP
It is an active metabolite of the selective estrogen receptor modulator (SERM) tamoxifen. Unlike tamoxifen, norendoxifen is not a SERM, and instead has been found to act as a potent and selective competitive inhibitor of aromatase (Kᵢ = 35 nM). Drugs with dual SERM and AI activity, such as 4'-hydroxynorendoxifen, have been developed from norendoxifen, and may have therapeutic potential as antiestrogens in the treatment of estrogen receptor-positive breast cancer.[1]
Chemistry
Harm reduction information
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Sources
- Journal / agency Lu WJ, Xu C, Pei Z, Mayhoub AS, Cushman M, Flockhart DA. The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents. Breast Cancer Research and Treatment. May 2012. doi:10.1007/s10549-011-1699-4 · PMID 21814747
- Journal / agency Lv W, Liu J, Skaar TC, Flockhart DA, Cushman M. Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities. Journal of Medicinal Chemistry. March 2015. doi:10.1021/jm501218e · PMID 25751283 · PMC4687028
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