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Drug

Afimoxifene

Established medicine
ClassEstrogen receptor modulatorResearchOngoing clinical research

Also known as 4-OHT, 4-hydroxytamoxifen, 4-monohydroxytamoxifen.

RxNorm1465159ChEMBLCHEMBL489UNII95K54647BZ
1
Active clinical trials
3
Protein targets
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

A Phase II Study of the Determinants of Transdermal Drug Delivery to the Normal and the Radiated Breast

Clinical trial2026-01-31Primary completion · ClinicalTrials.gov

Phase IIB Pre-Surgical Trial of Oral Tamoxifen Versus Transdermal 4-hydroxytamoxifen in Women With DCIS of the Breast

Clinical trial2024-12-18Results posted · ClinicalTrials.gov

A Randomized, Double-Blind, Placebo-Controlled Study of 4-hydroxytamoxifen Topical Gel in Women With Mammographically Dense Breast

Clinical trial2024-02-22Results posted · ClinicalTrials.gov

Pre-surgical Phase IIb Trial of Transdermal 4-Hydroxytamoxifen vs. Oral Tamoxifen in Women With Ductal Carcinoma in Situ of the Breast

Clinical trial2015-07-21Results posted · ClinicalTrials.gov

A Prospective, Randomized, Placebo-Controlled Trial of the Effects of 4-Hydroxytamoxifen Gel on Breast Density, Salivary Sex Steroids, and Quality of Life in Premenopausal Women

Clinical trial2004-07-01Completed · ClinicalTrials.gov

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Afimoxifene
Aliases & brands
4-OHT4-hydroxytamoxifen4-monohydroxytamoxifen
RxNorm CUI
1465159
ChEMBL ID
CHEMBL489
UNII
95K54647BZ
Primary mechanism
Estrogen receptor modulator

Pharmacology & targets

3 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

Estrogen receptor
ESR1 · P03372
MODULATOREstrogen receptor modulator
Estrogen receptor beta
ESR2 · Q92731
MODULATOREstrogen receptor modulator
Estrogen-related receptor gamma
ESRRG · P62508
ANTAGONISTEstrogen-related receptor gamma antagonist

Clinical trials

5 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
5
registered trials across all phases
LATEST COMPLETION 2022
1
Active studies
1
Late-stage (III+)
4
Completed
PHASE DISTRIBUTIONn = 5
Phase 24Phase N / A1

Recent completions

Trials that read out recently, adding to the completed evidence base.

Phase IIB Pre-Surgical Trial of Oral Tamoxifen Versus Transdermal 4-hydroxytamoxifen in Women With DCIS of the Breast

CompletedPH IINorthwestern Universityn=1002022

A Randomized, Double-Blind, Placebo-Controlled Study of 4-hydroxytamoxifen Topical Gel in Women With Mammographically Dense Breast

CompletedPH IIM.D. Anderson Cancer Centern=1942021

Pre-surgical Phase IIb Trial of Transdermal 4-Hydroxytamoxifen vs. Oral Tamoxifen in Women With Ductal Carcinoma in Situ of the Breast

CompletedPH IINorthwestern Universityn=272011

A Prospective, Randomized, Placebo-Controlled Trial of the Effects of 4-Hydroxytamoxifen Gel on Breast Density, Salivary Sex Steroids, and Quality of Life in Premenopausal Women

CompletedN/ANorthwestern University2004
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • ClinicalTrials.gov — clinical trials