ins365
Clinical trial activity
13 trials · 4 clinical orgs · 0 marketing orgs
Earliest trial started Sep 1, 1999 (NCT00680108)
Timeline
Indications
Mechanism of action
- Purinergic receptor P2Y2AGONIST
P2RY2 agonist
- Purinergic receptor P2Y1AGONIST
Purinergic receptor P2Y1 agonist
Selective for P2Y receptors. Purinergic receptor P2Y2 is the proposed target but the drug is active against P2Y1, P2Y2, P2Y4 and P2Y4 which could also contribute to activity (order of binding affinity; P2Y2 = P2Y4 > P2Y6 > P2Y1).
- Pyrimidinergic receptor P2Y4AGONIST
Pyrimidinergic receptor P2Y4 agonist
Selective for P2Y receptors. Purinergic receptor P2Y2 is the proposed target but the drug is active against P2Y1, P2Y2, P2Y4 and P2Y4 which could also contribute to activity (order of binding affinity; P2Y2 = P2Y4 > P2Y6 > P2Y1).
- Pyrimidinergic receptor P2Y6AGONIST
Pyrimidinergic receptor P2Y6 agonist
Selective for P2Y receptors. Purinergic receptor P2Y2 is the proposed target but the drug is active against P2Y1, P2Y2, P2Y4 and P2Y4 which could also contribute to activity (order of binding affinity; P2Y2 = P2Y4 > P2Y6 > P2Y1).
Chemistry & pharmacology
SMILES
O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1- Mol. weight
- 790.31 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL221326 ↗
- ChEMBLCHEMBL1767408 ↗
Also known as
- de-089
- de-089
- diquafosol
- diquafosol
- diquafosol
- diquafosol
- diquafosol
- diquafosol
- diquafosol
- diquafosol sodium
- diquafosol tetrasodium
- diquafosol tetrasodium
- diquafosol tetrasodium
- diquafosol tetrasodium
- diuridine 5'-(pentahydrogen tetraphosphate) tetrasodium salt
- ins365
- ins365
- ins365
- ins365
- ins 365
- ins-365
- ins-365
- ins-365
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02608489 | N/A | Jan 1, 2014 | Soonchunhyang University |
| NCT01240382 | Phase 3 | Nov 12, 2010 | Santen Inc. |
| NCT01189032 | Phase 2 | Aug 24, 2010 | Santen Inc. |
| NCT01101984 | N/A | Feb 1, 2010 | Santen Inc. |
| NCT00831662 | Phase 3 | Jan 1, 2009 | Inspire Pharmaceuticals, Merck |
| NCT00600288 | Phase 3 | Jan 1, 2008 | Merck |
| NCT01381731 | Phase 2 | Apr 1, 2005 | Merck |
| NCT00403975 | Phase 3 | Jun 1, 2004 | Merck |
| NCT00037661 | Phase 3 | Apr 1, 2002 | Merck |
| NCT00404131 | Phase 3 | Mar 1, 2001 | Merck |
| NCT00403715 | Phase 3 | Feb 1, 2001 | Merck |
| NCT00679718 | Phase 2 | Jan 1, 2000 | Merck |
| NCT00680108 | Phase 2 | Sep 1, 1999 | Merck |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 9 | 9 | 2 | 1999 |
| Santen Inc. | For profit | 3 | 3 | 3 | 2010 |
| Inspire Pharmaceuticals | For profit | 1 | 0 | 1 | 2009 |
| Soonchunhyang University | Academic/Hospital | 1 | 1 | 1 | 2014 |