galeterone
Small moleculeexperimental
Galeterone is a steroidal antiandrogen which was under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique triple mechanism of action, acting as an androgen receptor antagonist, androgen receptor down regulator, and CYP17A1 inhibitor, the latter of which prevents the biosynthesis of androgens. As a CYP17A1 inhibitor, galeterone shows selectivity for 17,20-lyase over 17α-hydroxylase. — Wikipedia
Clinical trial activity
5 trials · 4 clinical orgs · 0 marketing orgs
Phase 1
2
Phase 2
3
Phase 3
1
Phase 4
0
Earliest trial started Oct 1, 2009 (NCT00959959)
Timeline
Indications
Mechanism of action
- Androgen ReceptorANTAGONIST
AR antagonist
- Cytochrome P450 17A1INHIBITOR
CYP17A1 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(n3cnc4ccccc43)=CC[C@@H]12- Mol. weight
- 388.56 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaGaleterone ↗
- ChEMBLCHEMBL2105738 ↗
Also known as
- 17-(1h-benzimidazol-1-yl)androsta-5,16-dien-3beta-ol
- 3beta-hydroxy-17-(1h-benzimidazole-1-yl)androsta-5,16-diene
- 3-hydroxy-17-(1h-benzimidazole-1-yl)androsta-5,16-diene
- galeterone
- galeterone
- galeterone
- galeterone
- galeterone
- tok-001
- tok-001
- tok-001
- tok-001
- vn/124
- vn/124
- vn-124-1
- vn/124-1
- vn/124-1
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04098081 | Phase 2 | Nov 1, 2019 | University of Maryland |
| NCT02729376 | Phase 1 | Mar 1, 2016 | Novus Pharma |
| NCT02438007 | Phase 3 | Jun 1, 2015 | Novus Pharma |
| NCT01709734 | Phase 2 | Dec 1, 2012 | Harvard University, Novus Pharma, University of Washington |
| NCT00959959 | Phase 1 | Oct 1, 2009 | Harvard University, Novus Pharma, University of Washington |
Showing 5 of 5 trials
Page 1 / 1
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novus Pharma | For profit | 4 | 4 | 3 | 2009 |
| Harvard University | Academic/Hospital | 2 | 0 | 2 | 2009 |
| University of Washington | Academic/Hospital | 2 | 0 | 2 | 2009 |
| University of Maryland | Academic/Hospital | 1 | 1 | 1 | 2019 |
4 organizations
Page 1 / 1