irosustat
Irosustat is an orally active, irreversible, nonsteroidal inhibitor of steroid sulfatase (STS) and member of the aryl sulfamate ester class of drugs that was under development by Sterix Ltd and Ipsen for the treatment of hormone-sensitive cancers such as breast cancer, prostate cancer, and endometrial cancer but has not yet been marketed. The drug was first designed and synthesized in the group of Professor Barry V L Potter at the Department of Pharmacy & Pharmacology, University of Bath, working together with Professor Michael J. Reed at Imperial College, London and its initial development was undertaken through the university spin-out company Sterix Ltd and overseen by Cancer Research UK (CRUK). Results of the "first-in-class" clinical trial in breast cancer of an STS inhibitor in humans were published in 2006 and dose optimisation studies and further clinical data have been reported. — Wikipedia
Clinical trial activity
7 trials · 6 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2007 (NCT01840488)
Timeline
Indications
Mechanism of action
- Steryl-sulfataseINHIBITOR
STS inhibitor
Chemistry & pharmacology
SMILES
NS(=O)(=O)Oc1ccc2c3c(c(=O)oc2c1)CCCCC3- Mol. weight
- 309.34 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaIrosustat ↗
- ChEMBLCHEMBL286738 ↗
Also known as
- 667 coumate
- 667 coumate
- 667 coumate
- 6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta-(c)(1)benzopyran-3-o-sulfamate
- 6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta[c][1]benzopyran-3-o-sulfamate
- 6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta[c][1]benzopyran-3-o-sulfamate
- bn83495
- bn83495
- bn83495
- bn-83495
- bn-83495
- irosustat
- irosustat
- irosustat
- irosustat
- irosustat
- stx64
- stx64
- stx-64
- stx-64
- stx64 compound
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01785992 | Phase 2 | Oct 1, 2012 | Cancer Research UK, University of London |
| NCT01662726 | Phase 2 | Aug 1, 2012 | Ipsen, National Institute for Health Research, United Kingdom, QPS, University of London, University of Southern California |
| NCT01230970 | Phase 2 | May 1, 2011 | Ipsen |
| NCT01251354 | Phase 2 | Nov 1, 2010 | Ipsen |
| NCT00910091 | Phase 2 | Aug 1, 2009 | Ipsen |
| NCT00790374 | Phase 1 | Jan 1, 2009 | Ipsen |
| NCT01840488 | Phase 1 | Apr 1, 2007 | Ipsen |
Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Ipsen | For profit | 6 | 5 | 2 | 2007 |
| University of London | Academic/Hospital | 2 | 2 | 1 | 2012 |
| Cancer Research UK | Academic/Hospital | 1 | 0 | 1 | 2012 |
| National Institute for Health Research, United Kingdom | Government | 1 | 0 | 1 | 2012 |
| QPS | For profit | 1 | 0 | 1 | 2012 |
| University of Southern California | Academic/Hospital | 1 | 0 | 1 | 2012 |