Table 10.
Competitive and non-competitive AMPAR/KAR antagonists that have entered clinical trials in the last 15 years [38].
| Disease | Target/Mechanism | Drug | Stage of Development |
|---|---|---|---|
| Neuropathic Pain | Competitive GluK1 antagonist |
LY 5,454,694 tosylate |
Phase II (compl. 2010) |
| Competitive AMPAR/GluK1 antagonist |
NGX426 (tezampanel prodrug) |
Phase I (compl. 2008) | |
| Competitive AMPAR/KA antagonist |
NS 1209 | Phase II (compl. 2007) | |
| Competitive AMPAR/GluK1 antagonist |
Tezampanel (NGX424 LY 293558) | Phase I | |
| Migraine | Competitive AMPAR/GluK1 antagonist |
Tezampanel | Phase II (compl. 2009) |
| Competitive AMPAR antagonist |
Selurampanel | Phase II (compl. 2012) | |
| Non-competitive KAR antagonist |
Topiramate | Phase IV (compl. 2015) | |
| Epilepsy | Competitive AMPAR antagonist |
Becampanel | Phase II (compl. 2011) |
| Competitive AMPAR antagonist |
Selurampanel | Phase II (compl. 2012) | |
| Competitive AMPAR antagonist |
NS 1209 | Phase II | |
| Non-competitive KAR antagonist |
Topiramate | Phase IV (compl. 2010) | |
| Non-competitive AMPAR/KAR antagonist |
Perampanel | Marketed 2012 | |
| Non-competitive AMPAR antagonist |
Talampanel | Phase II (compl. 2006) | |
| Stroke and Head Trauma | Competitive AMPAR antagonist |
ZK200775 | Phase II (dis) |
| Amyotrophic Lateral Sclerosis |
Non-competitive AMPAR antagonist |
Talampanel | Phase II (compl. 2010) |
| Non-competitive AMPAR/KAR antagonist |
Perampanel | Phase II (terminated 2021) | |
| Parkinson’s Disease | Non-competitive AMPAR antagonist |
Talampanel | Phase II (compl. 2006) |
| Non- competitive AMPAR/KAR antagonist |
Perampanel | Phase III (compl. 2012) | |
| Eating Disorder |
Non-competitive KAR antagonist |
Topiramate | Phase I (compl. 2018) |
| Obesity | Non-competitive KAR antagonist |
Topiramate | Phase II (compl. 2017) |
| Chronic Subjective Tinnitus |
Competitive AMPAR antagonist |
Selurampanel | Phase II (compl. 2012) |
| Tourette Syndrome | Non-competitive KAR antagonist |
Topiramate | Phase III (compl. 2008) |
| Glial Brain Tumors |
Non-competitive AMPAR/KAR antagonist |
Perampanel | Phase IV (compl. 2017) |
| Non-competitive AMPAR antagonist |
Talampanel | Phase II (compl. 2011) | |
| Alcohol Dependence |
Non-competitive KAR antagonist |
Topiramate | Phase III (compl. 2011) |