afimoxifene
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. The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia of the breast. It has completed a phase II clinical trial for cyclical mastalgia, but further studies are required before afimoxifene can be approved for this indication and marketed. — Wikipedia
Clinical trial activity
8 trials · 6 clinical orgs · 0 marketing orgs
Earliest trial started Mar 1, 2003 (NCT00272714)
Timeline
Indications
Mechanism of action
- Estrogen-related receptor gammaANTAGONIST
ESRRG antagonist
Active metabolite of tamoxifen
- Estrogen receptorMODULATOR
Estrogen receptor modulator
Active metabolite of tamoxifen
Chemistry & pharmacology
SMILES
CC/C(=C(\c1ccccc1)c1ccc(OCCN(C)C)cc1)c1ccc(O)cc1- Mol. weight
- 387.52 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaAfimoxifene ↗
- ChEMBLCHEMBL489 ↗
- ChEMBLCHEMBL10041 ↗
Also known as
- 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol
- 4,17 beta-dihydroxy-4-androstene-3-one
- 4-androstene-7alpha-17beta-diol-3-one
- 4-hydroxytamoxifen
- 4-hydroxytamoxifen
- 4-hydroxytamoxifen
- 4-hydroxytamoxifen
- 4-hydroxy-tamoxifen
- 4'-hydroxytamoxifen
- 4-hydroxytamoxifen, (e)-isomer
- 4-hydroxytamoxifen, (z)-isomer
- 4-monohydroxytamoxifen
- 4-monohydroxytamoxifen
- 4-monohydroxytamoxifen
- 4-oht
- 4-oht
- 4-oht
- 4-oht
- 4oh-tamoxifen
- 4-oht hydrotamoxifen
- 7alpha-hydroxytestosterone
- afimoxifene
- afimoxifene
- afimoxifene
- afimoxifene
- afimoxifene
- androst-4-en-3-one, 4,17-dihydroxy-, (17beta)-
- (e)-4-hydroxytamoxifen
- ici 79280
- para-hydroxytamoxifen
- phenol, 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-butenyl)-
- phenol, 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-butenyl)-,
- tamogel
- tamogel
- tamoxifen metabolite b
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04570956 | Phase 2/Phase 3 (Phase 3) | Jul 26, 2021 | Mayo Clinic |
| NCT04009044 | Phase 2 | Jul 25, 2019 | National Cancer Institute (NCI), Northwestern University |
| NCT03199963 | Phase 3 | Aug 21, 2017 | Besins Healthcare |
| NCT02993159 | Phase 2 | Jun 1, 2017 | Besins Healthcare, Northwestern University |
| NCT03063619 | Phase 2 | May 30, 2017 | Besins Healthcare, University of Texas at Houston |
| NCT00952731 | Phase 2 | Dec 1, 2009 | National Cancer Institute (NCI), Northwestern University |
| NCT00084344 | N/A | Apr 1, 2003 | National Cancer Institute (NCI), Northwestern University |
| NCT00272714 | Phase 2 | Mar 1, 2003 | Besins Healthcare, University of Wales |
Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Besins Healthcare | For profit | 4 | 4 | 2 | 2003 |
| Northwestern University | Academic/Hospital | 4 | 3 | 2 | 2003 |
| National Cancer Institute (NCI) | Government | 3 | 0 | 2 | 2003 |
| Mayo Clinic | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Texas at Houston | Academic/Hospital | 1 | 0 | 1 | 2017 |
| University of Wales | Academic/Hospital | 1 | 0 | 1 | 2003 |