preladenant
Small moleculeexperimental
Preladenant is a drug that was developed by Schering-Plough which acts as a potent and selective antagonist of the adenosine A2A receptor. It was being researched as a potential treatment for Parkinson's disease. Positive results were reported in Phase II clinical trials in humans, but it did not prove itself to be more effective than a placebo during Phase III trials, and so was discontinued in May 2013. — Wikipedia
Clinical trial activity
13 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
4
Phase 2
9
Phase 3
4
Phase 4
0
Earliest trial started Jul 1, 2006 (NCT00686699)
Timeline
Indications
Studied for
- Akathisia, Drug-Induced · Phase 2
- Antipsychotic Agents · Phase 2
- Brain Diseases · Phase 2
- Central Nervous System Diseases · Phase 2
- Dyskinesia, Drug-Induced · Phase 2
- Liver Diseases · Phase 1
- Movement Disorders · Phase 2
- Neoplasms · Phase 1
- Neurodegenerative Diseases · Phase 2
- Parkinson Disease · Phase 3
- Parkinsonian Disorders · Phase 2
Mechanism of action
- Adenosine A2a receptorANTAGONIST
ADORA2A antagonist
Discontinued no more effective than placebo.
Chemistry & pharmacology
Loading structure…
SMILES
COCCOc1ccc(N2CCN(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1- Mol. weight
- 503.57 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPreladenant ↗
- ChEMBLCHEMBL240624 ↗
Also known as
- 2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine
- mk-3814
- mk-3814
- preladenant
- preladenant
- preladenant
- preladenant
- preladenant
- sch420814
- sch 420814
- sch 420814
- sch 420814
- sch-420814
- sch-420814
- sch-420814
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03099161 | Phase 1 | Jun 28, 2017 | Merck |
| NCT01465412 | Phase 1 | Nov 1, 2011 | Merck |
| NCT01323855 | Phase 1 | Mar 1, 2011 | Merck |
| NCT01294800 | Phase 2 | Feb 1, 2011 | Merck |
| NCT01227265 | Phase 3 | Nov 1, 2010 | Merck |
| NCT01215227 | Phase 3 | Nov 1, 2010 | Merck |
| NCT01155479 | Phase 3 | Jul 1, 2010 | Merck |
| NCT01155466 | Phase 3 | Jul 1, 2010 | Merck |
| NCT00845000 | Phase 1 | Apr 1, 2009 | Merck, Oregon Health and Science University |
| NCT00537017 | Phase 2 | Nov 1, 2007 | Merck |
| NCT00693472 | Phase 2 | Aug 15, 2007 | Merck |
| NCT00406029 | Phase 2 | Nov 1, 2006 | Merck |
| NCT00686699 | Phase 2 | Jul 1, 2006 | Merck |
Showing 13 of 13 trials
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Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 13 | 13 | 3 | 2006 |
| Oregon Health and Science University | Academic/Hospital | 1 | 0 | 1 | 2009 |
2 organizations
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