Clinical data
Synonyms N-Desmethyl-4-hydroxytamoxifen; 4-Hydroxy-N-desmethyltamoxifen; Desmethylhydroxytamoxifen
CAS Number
PubChem CID
PDB ligand
Chemical and physical data
Formula C25H27NO2
Molar mass 373.496 g/mol
3D model (JSmol)

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is an orally active nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that is or was under development for the treatment of estrogen receptor-positive breast cancer.[1][2][3][4] It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders.[5][6] Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant).[2][7][8][9] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.[10]

See also


  1. http://webcache.googleusercontent.com/search?q=cache:xvQZVuqnC0QJ:adisinsight.springer.com/drugs/800036114+&cd=1&hl=en&ct=clnk&gl=us
  2. 1 2 "Endoxifen shows promise as breast cancer treatment". Forefront. Mayo Clinic. 3 (1). 2014.
  3. Ahmad A, Ali SM, Ahmad MU, Sheikh S, Ahmad I (July 2010). "Orally administered endoxifen is a new therapeutic agent for breast cancer". Breast Cancer Research and Treatment. 122 (2): 579–84. doi:10.1007/s10549-009-0704-7. PMID 20052538.
  4. "Z-endoxifen hydrochloride". NCI Drug Dictionary.
  5. Ahmad A, Sheikh S, Shah T, Reddy MS, Prasad B, Verma KK, Chandrakant BB, Paithankar M, Kale P, Solanki RV, Patel R, Barkate H, Ahmad I (June 2016). "Endoxifen, a New Treatment Option for Mania: A Double-Blind, Active-Controlled Trial Demonstrates the Antimanic Efficacy of Endoxifen". Clinical and Translational Science. 9 (5): 252–9. doi:10.1111/cts.12407. PMID 27346789.
  6. Rankovic Z, Bingham M, Hargreaves R, eds. (2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. p. 349. ISBN 978-1-84973-365-6.
  7. Hawse JR, Subramaniam M, Cicek M, Wu X, Gingery A, Grygo SB, Sun Z, Pitel KS, Lingle WL, Goetz MP, Ingle JN, Spelsberg TC (2013). "Endoxifen's molecular mechanisms of action are concentration dependent and different than that of other anti-estrogens". PLoS One. 8 (1): e54613. Bibcode:2013PLoSO...854613H. doi:10.1371/journal.pone.0054613. PMC 3557294. PMID 23382923. Lay summary Medical Daily (December 12, 2013).
  8. Wu X, Hawse JR, Subramaniam M, Goetz MP, Ingle JN, Spelsberg TC (March 2009). "The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells". Cancer Research. 69 (5): 1722–7. doi:10.1158/0008-5472.CAN-08-3933. PMID 19244106.
  9. Gingery A, Subramaniam M, Pitel KS, Reese JM, Cicek M, Lindenmaier LB, Ingle JN, Goetz MP, Turner RT, Iwaniec UT, Spelsberg TC, Hawse JR (2014). "The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton". PLoS One. 9 (5): e98219. Bibcode:2014PLoSO...998219G. doi:10.1371/journal.pone.0098219. PMC 4031133. PMID 24853369.
  10. Wilcken N (2016). "Breast cancer: a disease of subtypes". Cancer Forum. 40 (3).

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