Trioxifene Explained

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] [3] [4]} Its affinity for the rat estrogen receptor was reported to be 20% relative to estradiol.^{[5] [6]}

Notes and References

1. Neubauer BL, McNulty AM, Chedid M, Chen K, Goode RL, Johnson MA, Jones CD, Krishnan V, Lynch R, Osborne HE, Graff JR . 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 . September 2003 . 14522935 .
2. Book: Maximov PY, McDaniel RE, Jordan VC . Tamoxifen: Pioneering Medicine in Breast Cancer. . Milestones in Drug Therapy . Springer Science & Business Media . 2013 . 978-3-03-480664-0 .
3. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 14 November 2014. Springer. 978-1-4757-2085-3. 1252–.
4. Book: Morton IK, Hall JM . Concise Dictionary of Pharmacological Agents: Properties and Synonyms. 6 December 2012. Springer Science & Business Media. 978-94-011-4439-1. 281–.
5. Chander SK, Sahota SS, Evans TR, Luqmani YA . The biological evaluation of novel antioestrogens for the treatment of breast cancer . Crit Rev Oncol Hematol . 15 . 3 . 243–69 . December 1993 . 8142059 . 10.1016/1040-8428(93)90044-5 .
6. Book: Kelce WR, Gray Jr LE . Endocrine Disruptors: Effects on Sex Steroid Hormone Receptors and Sex Development . Kavlock RJ, Daston GP . Drug Toxicity in Embryonic Development II: Advances in Understanding Mechanisms of Birth Defects: Mechanistics Understanding of Human Development Toxicants. https://books.google.com/books?id=vcHsCAAAQBAJ&pg=PA437 . 6 December 2012 . Springer Science & Business Media . 978-3-642-60447-8 . 437–.