Afimoxifene

Afimoxifene
Clinical data
Synonyms 4-Hydroxytamoxifen; 4-OHT; 4-HT; OHTAM; TamoGel
Routes of
administration		 Topical (gel)
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.155.464 Edit this at Wikidata
Chemical and physical data
Formula C26H29NO2
Molar mass 387.5139 g/mol
3D model (JSmol)
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Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT, 4-HT, OHTAM, others), is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and the major active metabolite of tamoxifen.[1][2][3] The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia of the breast.[1][4] It has completed a phase II clinical trial for cyclical mastalgia,[5] but further studies are required before afimoxifene can be approved for this indication and marketed.[4]

A study in France on 55 women showed that rubbing afimoxifene on the skin was as effective as oral tamoxifen at slowing breast cancer growth. A United States trial will compare 6 weeks use before breast cancer surgery. Skin application can reduce systemic levels by a factor of nine and this is expected to reduce the unpleasant side-effects of tamoxifen.

In addition to its antiestrogenic and estrogenic activity, afimoxifene has been found to act as an antagonist of the estrogen-related receptors (ERRs) ERRβ and ERRγ.[6][7]

See also

References

  1. 1 2 http://adisinsight.springer.com/drugs/800019175
  2. ↑ Desta Z, Ward BA, Soukhova NV, Flockhart DA (2004). "Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6". J Pharmacol Exp Ther. 310 (3): 1062–1075. doi:10.1124/jpet.104.065607. PMID 15159443.
  3. ↑ "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene" (PDF). American Medical Association. Retrieved 2008-03-26.
  4. 1 2 Ismail Jatoi; Achim Rody (16 November 2016). Management of Breast Diseases. Springer. pp. 77–. ISBN 978-3-319-46356-8.
  5. ↑ Mansel R, Goyal A, Nestour EL, Masini-Etévé V, O'Connell K (2007). "A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women". Breast Cancer Res. Treat. 106 (3): 389–397. doi:10.1007/s10549-007-9507-x. PMID 17351746.
  6. ↑ Alice C. Levine (3 October 2011). Hormones and Cancer: Breast and Prostate, An Issue of Endocrinology and Metabolism Clinics of North America,. Elsevier Health Sciences. pp. 271–. ISBN 1-4557-1239-6.
  7. ↑ Sushil K. Khetan (23 May 2014). Endocrine Disruptors in the Environment. Wiley. pp. 104–. ISBN 978-1-118-89115-5.



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