Chemistry:N-Desmethyltamoxifen
From HandWiki
Short description: Chemical compound
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| Other names | ICI-55,548; Nortamoxifen; NDMTAM |
| Drug class | Selective estrogen receptor modulator |
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| Formula | C25H27NO |
| Molar mass | 357.497 g·mol−1 |
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N-Desmethyltamoxifen (developmental code name ICI-55,548) is a major metabolite of tamoxifen, a selective estrogen receptor modulator (SERM).[1][2] N-Desmethyltamoxifen is further metabolized into endoxifen (4-hydroxy-N-desmethyltamoxifen), which is thought to be the major active form of tamoxifen in the body.[1][2][3] In one study, N-desmethyltamoxifen had an affinity for the estrogen receptor of 2.4% relative to estradiol.[4] For comparison, tamoxifen, endoxifen, and afimoxifene (4-hydroxytamoxifen) had relative binding affinities of 2.8%, 181%, and 181%, respectively.[4]
References
- ↑ 1.0 1.1 "Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen". Expert Review of Clinical Pharmacology 12 (6): 523–536. June 2019. doi:10.1080/17512433.2019.1610390. PMID 31008668.
- ↑ 2.0 2.1 "PharmGKB summary: tamoxifen pathway, pharmacokinetics". Pharmacogenet Genomics 23 (11): 643–7. November 2013. doi:10.1097/FPC.0b013e3283656bc1. PMID 23962908.
- ↑ "Individualization of tamoxifen therapy: much more than just CYP2D6 genotyping". Cancer Treat Rev 41 (3): 289–99. March 2015. doi:10.1016/j.ctrv.2015.01.002. PMID 25618289.
- ↑ 4.0 4.1 "Pharmacological relevance of endoxifen in a laboratory simulation of breast cancer in postmenopausal patients". J Natl Cancer Inst 106 (10). October 2014. doi:10.1093/jnci/dju283. PMID 25258390.
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