Quote:
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Conclusions: We have demonstrated in both ER+ and ER+/HER2+ breast cancer cell lines that in contrast to Tam, endoxifen potently inhibits growth (both in vitro and in vivo), does not activate Erk1/2 signaling, and inhibits E2-stimulated transcription of ER-regulated genes. Endoxifen exhibited potent antitumor activity in MCF7-HER2 xenografts refractory to Tam. These data support the ongoing NCI sponsored phase I studies of Z-endoxifen at Mayo Clinic and NCI.
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Tamoxifen effectiveness is determined by ability of a body to turn it into/metabolize to endoxifen. It's a pro-drug for endoxifen.
http://www.sciencedaily.com/releases...1211141838.htm
So I guess this article is suggesting some of the acquired resistance to TAM is due to a change in the metabolism/transformation of TAM...as opposed to resistance to TAM as a drug.
Linear Mode
