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Trioxifene

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Trioxifene
Clinical data
Other namesLY-133,314
Routes of
administration		Oral
ATC code
  • none
Identifiers
  • [2-(4-methoxyphenyl)-3,4-dihydronaphthalen-1-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC30H31NO3
Molar mass453.582 g·mol−1

Trioxifene (INN; developmental code LY-133,314), or as the salt trioxifene mesylate (USAN), is a selective estrogen receptor modulator (SERM) with competitive binding activity against estradiol for the ERα and antagonistic activity against ERα-mediated gene expression, that was under preclinical and clinical development by Eli Lilly and Company for breast cancer and prostate cancer,[1] but was abandoned.[2]: 11 [3][4] Its affinity for the rat estrogen receptor was reported to be 20% relative to estradiol.[5][6]

References

  1. ^ Neubauer BL, McNulty AM, Chedid M, Chen K, Goode RL, Johnson MA, Jones CD, Krishnan V, Lynch R, Osborne HE, Graff JR (September 2003). "The selective estrogen receptor modulator trioxifene (LY133314) inhibits metastasis and extends survival in the PAIII rat prostatic carcinoma model". Cancer Research. 63 (18): 6056–62. PMID 14522935.
  2. ^ Maximov PY, McDaniel RE, Jordan VC (2013). "Tamoxifen: Pioneering Medicine in Breast Cancer.". Milestones in Drug Therapy. Springer Science & Business Media. ISBN 978-3-03-480664-0.
  3. ^ Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 1252–. ISBN 978-1-4757-2085-3.
  4. ^ Morton IK, Hall JM (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 281–. ISBN 978-94-011-4439-1.
  5. ^ Chander SK, Sahota SS, Evans TR, Luqmani YA (December 1993). "The biological evaluation of novel antioestrogens for the treatment of breast cancer". Crit Rev Oncol Hematol. 15 (3): 243–69. doi:10.1016/1040-8428(93)90044-5. PMID 8142059.
  6. ^ Kelce WR, Gray Jr LE (6 December 2012). "Endocrine Disruptors: Effects on Sex Steroid Hormone Receptors and Sex Development". In Kavlock RJ, Daston GP (eds.). Drug Toxicity in Embryonic Development II: Advances in Understanding Mechanisms of Birth Defects: Mechanistics Understanding of Human Development Toxicants. Springer Science & Business Media. pp. 437–. ISBN 978-3-642-60447-8.



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