tezampanel
Tezampanel is a drug originally developed by Eli Lilly which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant properties, the former of which may, at least in part, occur via blockade of calcium uptake into neurons. — Wikipedia
Clinical trial activity
1 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2006 (NCT00567086)
Timeline
2000s
- Jan 1, 2006
Earliest Phase 2 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Glutamate receptor ionotropic kainateANTAGONIST
Glutamate receptor ionotropic kainate antagonist
Active metabolite of oral prodrug NGX424. AMPA/Kainate receptor antagonist, selective for GRIK1 subunit containing receptors. Indication: Migraine, Postoperative pain
- Glutamate receptor ionotropic AMPAANTAGONIST
Glutamate receptor ionotropic AMPA antagonist
Active metabolite of oral prodrug NGX424. AMPA/Kainate receptor antagonist, selective for GRIK1 subunit containing receptors. Indication: Migraine, Postoperative pain
Chemistry & pharmacology
SMILES
O.O=C(O)[C@@H]1C[C@H]2C[C@@H](CCc3nn[nH]n3)CC[C@H]2CN1- Mol. weight
- 297.36 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL3989703 ↗
- WikipediaTezampanel ↗
- ChEMBLCHEMBL14935 ↗
Also known as
- (3s,4ar,6r,8ar)-6-(2-(1(2)h-tetrazole-5yl)ethyl)decahydroisoquinoline-3carboxylic acid
- 6-(2-(1h-tetrazol-5-yl)ethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
- ly 215490
- ly-215490
- ly293558
- ly 293558
- ly-293558
- ly-293558
- ly-293558
- ly 326325
- ly-326325
- ngx424
- ngx424
- ngx424
- tezampanel
- tezampanel
- tezampanel
- tezampanel
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00567086 | Phase 2 | Oct 1, 2006 | TorreyPines Therapeutics |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| TorreyPines Therapeutics | For profit | 1 | 1 | 1 | 2006 |