rolofylline
Small moleculeexperimental
Rolofylline (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist. It was discovered at NovaCardia, Inc. which was purchased by Merck & Co., Inc. in 2007. — Wikipedia
Clinical trial activity
7 trials · 5 clinical orgs · 0 marketing orgs
Phase 1
0
Phase 2
7
Phase 3
3
Phase 4
0
Earliest trial started Aug 1, 2004 (NCT00159627)
Timeline
Indications
Mechanism of action
- Adenosine A1 receptorANTAGONIST
ADORA1 antagonist
Discontinued no more effective than placebo.
Chemistry & pharmacology
Loading structure…
SMILES
CCCn1c(=O)c2nc(C34CC5CC(CC3C5)C4)[nH]c2n(CCC)c1=O- Mol. weight
- 356.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL52333 ↗
- WikipediaRolofylline ↗
- ChEMBLCHEMBL2103819 ↗
Also known as
- 1,3-dipropyl-8-(3-noradamantyl)xanthine
- 1,3-dnax
- 8-(3-noradamantyl)-1,3-dipropylxanthine
- 8-(noradamantan-3-yl)-1,3-dipropylxanthine
- kw 3902
- kw-3902
- kw-3902
- kw-3902
- kw-3902
- mk7418
- mk 7418
- mk-7418
- mk-7418
- mk-7418
- rolofylline
- rolofylline
- rolofylline
- rolofylline
- rolofylline
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00729222 | Phase 2 | Nov 1, 2008 | Merck, NovaCardia |
| NCT00443690 | Phase 3 | Aug 1, 2007 | Duke University, Merck, NovaCardia, University of California, San Francisco |
| NCT00354458 | Phase 3 | Oct 1, 2006 | Duke University, Merck, NovaCardia, University of Brescia, University of California, San Francisco |
| NCT00328692 | Phase 3 | Aug 1, 2006 | Duke University, Merck, NovaCardia, University of Brescia, University of California, San Francisco |
| NCT00159614 | Phase 2 | Sep 1, 2005 | Merck, NovaCardia |
| NCT00652782 | Phase 2 | Dec 1, 2004 | Merck, NovaCardia |
| NCT00159627 | Phase 2 | Aug 1, 2004 | Merck, NovaCardia |
Showing 7 of 7 trials
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Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 7 | 1 | 2 | 2004 |
| NovaCardia | For profit | 7 | 6 | 2 | 2004 |
| Duke University | Academic/Hospital | 3 | 0 | 1 | 2006 |
| University of California, San Francisco | Academic/Hospital | 3 | 0 | 1 | 2006 |
| University of Brescia | Academic/Hospital | 2 | 0 | 1 | 2006 |
5 organizations
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