irampanel
Irampanel is a drug which acts as a dual noncompetitive antagonist of the AMPA receptor and neuronal voltage-gated sodium channel blocker. It was under development by Boehringer Ingelheim for the treatment of acute stroke/cerebral ischemia but never completed clinical trials for this indication. Irampanel was also trialed, originally, for the treatment of epilepsy and pain, but these indications, too, were abandoned, and the drug was ultimately never marketed. — Wikipedia
Clinical trial activity
3 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 1999 (NCT02222974)
Timeline
1990s
- Jan 1, 1999
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Glutamate receptor ionotropic AMPAANTAGONIST
Glutamate receptor ionotropic AMPA antagonist
Non-competitive AMPA receptor antagonist.
- Sodium channel alpha subunitBLOCKER
Sodium channel alpha subunit blocker
- Sodium channel protein type 1 subunit alpha (SCN1A) ↗
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗
- Sodium channel protein type 7 subunit alpha (SCN7A) ↗
- Sodium channel protein type 2 subunit alpha (SCN2A) ↗
- Sodium channel protein type 9 subunit alpha (SCN9A) ↗
- Sodium channel protein type 3 subunit alpha (SCN3A) ↗
- Sodium channel protein type 11 subunit alpha (SCN11A) ↗
- Sodium channel protein type 8 subunit alpha (SCN8A) ↗
- Sodium channel protein type 10 subunit alpha (SCN10A) ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type VII alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
Chemistry & pharmacology
SMILES
CN(C)CCOc1ccccc1-c1nc(-c2ccccc2)no1- Mol. weight
- 309.37 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaIrampanel ↗
- ChEMBLCHEMBL29741 ↗
Also known as
- biir-561
- biir-561
- biir 561 cl
- biir 561 cl
- biir 561 cl
- biir-561cl
- biir-561 cl
- biir-561 cl
- dimethyl-(2-(2-(3-phenyl-(1,2,4)oxadiazol-5-yl)phenoxy)ethyl)amine hydrochloride
- irampanel
- irampanel
- irampanel
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02223507 | Phase 1 | Aug 1, 2000 | Boehringer Ingelheim |
| NCT02222961 | Phase 1 | Nov 1, 1999 | Boehringer Ingelheim |
| NCT02222974 | Phase 1 | Jan 1, 1999 | Boehringer Ingelheim |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 3 | 3 | 1 | 1999 |