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| Clinical data | |
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| Trade names | TamoGel |
| Other names | 4-Hydroxytamoxifen; 4-OHT; 4-HT; OHTAM; TamoGel |
| Routes of administration | Topical (gel) |
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| UNII | |
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| ECHA InfoCard | 100.163.120 |
| Chemical and physical data | |
| Formula | C26H29NO2 |
| Molar mass | 387.523 g·mol−1 |
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Afimoxifene, also known as4-hydroxytamoxifen (4-OHT) and by its tentative brand nameTamoGel, is aselective estrogen receptor modulator (SERM) of thetriphenylethylene group and anactive metabolite oftamoxifen.[1][2][3] The drug is under development under the tentative brand nameTamoGel as atopical gel for the treatment ofhyperplasia of thebreast.[1][4] It has completed aphase IIclinical trial forcyclical mastalgia,[5] but further studies are required before afimoxifene can be approved for this indication and marketed.[4]
Afimoxifene is a SERM and hence acts as atissue-selectiveagonist–antagonist of theestrogen receptorsERα andERβ with mixedestrogenic andantiestrogenic activity depending on thetissue. It is also anagonist of theG protein-coupled estrogen receptor (GPER) with relatively lowaffinity (100–1,000 nM, relative to 3–6 nM forestradiol).[6] In addition to its estrogenic and antiestrogenic activity, afimoxifene has been found to act as anantagonist of theestrogen-related receptors (ERRs)ERRβ andERRγ.[7][8][9]
