Afimoxifene

DB04468InvestigationalSmall molecule

Afimoxifene (4-Hydroxytamoxifen, trade name TamoGel) is a new estrogen inhibitor under investigation for a variety of estrogen-dependent conditions, including cyclic breast pain and gynecomastia. TamoGel is formulated using Enhanced Hydroalcoholic... This technology enables percutaneous delivery of drugs that cannot be delivered orally.

Mechanism: Afimoxifene binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes.
Curator reviewed
Primary indication: For the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.Curator reviewed
Formula / weight: C₂₆H₂₉NO₂ · 387.514 g/mol (avg)
Also known as: 4-hydroxytamoxifen · 4-monohydroxytamoxifen · 4-OHT
Code names: 68047-06-3 · ICI-79280

Resolves to

Compound

UNII95K54647BZCAS68392-35-8ChEMBLCHEMBL489ChEBI44616PubChem449459KEGGD06551

Structure

InChIKeyTXUZVZSFRXZGTL-QPLCGJKRSA-NSMILESCC\C(=C(/C1=CC=C(O)C=C1)C1=CC=C(OCCN(C)C)C=C1)C1=CC=CC=C1

Targets

P03372ESR1P62508ESRRGP04155TFF1P11474ESRRAO75469NR1I2P04278SHBGQ92731ESR2

What you can answer from here — as of September 23, 2026

8Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

41Drug interactionsStructured to mechanism, not free text

9Clinical trialsPhase, status and sponsor resolved per trial

30+ReferencesStructured and connected to the statements they support

Which drugs share a target with Afimoxifene, and which of those have an active Phase 3 trial?

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