Table 2.
Centrally-Acting Anti-Obesity Drugs
| Target | Drug | Mechanism of Action |
Company | Status |
|---|---|---|---|---|
| NPY | MK-0557 | Y5 receptor antagonist | Merck | Phase II |
| S-2367 | Y5 receptor antagonist | Shionogi USA, Inc. | Phase II | |
| AgRP | TTT-435 | AgRP inhibitor | TransTech Pharma | Phase II |
| MCH | BMS-830216 | MCH-1 receptor antagonist | Bristol-Myers Squibb | Phase I/II |
| CCK | GI 181771X | Selective CCK-A agonist | Glaxo Smith Kline | Terminated |
| GLP-1 | Vildagliptin | DDP-IV inhibitor | Novartis | Phase III |
| Sitagliptin | DDP-IV inhibitor | Merck | Approved for Diabetes | |
| Liraglutide | Proteolysis resistant GLP-1 analogue | Novo Nordisk | Approved for Diabetes | |
| Exenatide | Proteolysis resistant GLP-1 analogue | Amylin/Eli Lilly | Approved for Diabetes | |
| Exenatide-LAR | Long-acting proteolysis resistant GLP-1 analogue | Amylin/Eli Lilly | FDA Regulatory Review | |
| NN9924 | Long-acting oral GLP-1 analogue | Novo Nordisk | Phase I | |
| Oxyntomodulin (OXM) | TKS1225 | Long-acting OXM analogue | Thiakis, Ltd./Wyeth/Pfizer | Pre-Clinical |
| PYY | PYY (3–36) | Intranasal active PYY | Nastech/Merck | Phase I/II |
| Ghrelin | NOX-B11 | Ghrelin inactivator | NOXXON Pharma Ag/Pfizer | Pre-Clinical |
| Oral Ghrelin Antagonist | Ghrelin antagonist | Elixir Pharmaceuticals | Pre-Clinical | |
| Pancreatic polypeptide (PP) | Obinepitide | Y2/Y4 receptor agonist | 7TM Pharma | Phase I/II |
| TM30339 | Selective Y4 receptor agonist | 7TM Pharma | Phase I/II | |
| Amylin | Pramlintide | Synthetic amylin analogue | Amylin Pharmaceuticals | Approved for Diabetes |
| Leptin | Metreleptin/Pramlintide | Leptin/amylin analogues | Amylin Pharmaceuticals | Phase II |
| 5HT2C Receptor | Lorcaserin HCl | 5HT2C agonist | Arena Pharmaceuticals, Inc. | FDA Review |
| H1/H3 Receptor | SCH-497079 | H3 receptor antagonist | Schering-Plough | Phase II |
| Histalean | H1-receptor agonist/H3 receptor antagonist | OBEcure, Ltd. | Phase II | |
| Noradrenergic, Dopaminergic, & Opioid Signaling | Contrave (Bupropion-SR + Naltrexone) | Norepinephrine- and dopamine-reuptake inhibitor/μ-opioid receptor antagonist | Orexigen Therapeutics, Inc. | Phase III |
| Noradrenergic, Dopaminergic, & GABA Signaling | Empatic (Bupropion-SR + Zonisamide) | Norepinephrine- and dopamine-reuptake inhibitor/GABA receptor activator | Orexigen Therapeutics, Inc. | Phase III |
| Noradrenergic & GABA Signaling | Qnexa (Topiramate + Phentermine) | Norepinephrine releasing agent/GABA receptor activator | Vivus, Inc. | Phase III |