Afimoxifene
Chemical compound
From Wikipedia, the free encyclopedia
Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an 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]
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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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| ECHA InfoCard | 100.163.120 |
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| Formula | C26H29NO2 |
| Molar mass | 387.523 g·mol−1 |
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Afimoxifene is a SERM and hence acts as a tissue-selective agonist–antagonist of the estrogen receptors ERα and ERβ with mixed estrogenic and antiestrogenic activity depending on the tissue. It is also an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100–1,000 nM, relative to 3–6 nM for estradiol).[6] In addition to its estrogenic and antiestrogenic activity, afimoxifene has been found to act as an antagonist of the estrogen-related receptors (ERRs) ERRβ and ERRγ.[7][8][9]