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Endoxifen

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Endoxifen
Clinical data
Other names(Z)-endoxifen; Z-endoxifen HCl
Identifiers
  • 4-[(Z)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.208.548 Edit this at Wikidata
Chemical and physical data
FormulaC25H27NO2
Molar mass373.496 g/mol g·mol−1

Endoxifen is an orally active, selective estrogen receptor modulator (SERM) that was developed for the treatment of estrogen receptor-positive breast cancer.[1][2][3] Endoxifen is a metabolite of tamoxifen and is shown to be effective in patients that have failed previous hormonal therapies (aromatase inhibitors, fulvestrant and tamoxifen). [1] [4] [5] [6] The prodrug tamoxifen is metabolized by CYP2D6 enzyme to produce endoxifen. [7]

Endoxifen is also being evaluated as an anti-psychotic for treatment of mania and other psychotic disorders.[8] [9]

References

  1. ^ a b "Endoxifen shows promise as breast cancer treatment". No. Vol. 3, Issue 1, 2014. FOREFRONT: MAYO CLINIC CANCER CENTER'S ONLINE MAGAZINE. {{cite news}}: |issue= has extra text (help)
  2. ^ Ahmad, Ateeq, Shoukath M. Ali, Moghis U. Ahmad, Saifuddin Sheikh, and Imran Ahmad. "Orally administered endoxifen is a new therapeutic agent for breast cancer". Breast cancer research and treatment (122, no. 2 (2010):): 579-584.{{cite journal}}: CS1 maint: extra punctuation (link) CS1 maint: multiple names: authors list (link)
  3. ^ "NCI Drug Dictionary".
  4. ^ John Ericson (Dec 12, 2013). "New Breast Cancer Drug Endoxifen Shows Promise In Patients Resistant To Conventional Hormonal Therapy: Trial". Medical Daily.
  5. ^ Wu, Xianglin, John R. Hawse, Malayannan Subramaniam, Matthew P. Goetz, James N. Ingle, and Thomas C. Spelsberg. "The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor α for degradation in breast cancer cells." Cancer research 69, no. 5 (2009): 1722-1727. http://cancerres.aacrjournals.org/content/69/5/1722
  6. ^ Gingery, Anne, Malayannan Subramaniam, Kevin S. Pitel, Jordan M. Reese, Muzaffer Cicek, Laurence B. Lindenmaier, James N. Ingle et al. "The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton." PloS one 9, no. 5 (2014): e98219.
  7. ^ Wilcken, Nicholas. "Breast cancer: a disease of subtypes." Breast cancer 40 (2016). http://cancerforum.org.au/forum/2016/november/breast-cancer-a-disease-of-subtypes/
  8. ^ Ahmad, A., S. Sheikh, T. Shah, M. S. Reddy, B. S. V. Prasad, K. K. Verma, B. B. Chandrakant et al. "Endoxifen, a New Treatment Option for Mania: A Double‐Blind, Active‐Controlled Trial Demonstrates the Antimanic Efficacy of Endoxifen." Clinical and Translational Science 9, no. 5 (2016): 252-259. http://www.ncbi.nlm.nih.gov/pubmed/27346789
  9. ^ Rankovic, Zoran, Richard Hargreaves, and Matilda Bingham, (2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. p. 349.{{cite book}}: CS1 maint: extra punctuation (link) CS1 maint: multiple names: authors list (link)
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