TABLE 1.
New molecular entities targeting GPCRs in 2014
MOR, μ-opioid receptor.
| Drug name | GPCR | Indication | Ref. |
|---|---|---|---|
| Tasimelteon | MT1/MT2 melatonin receptor agonist | Non-24-hour sleep-wake disturbance | 60 |
| Droxidopa | Adrenergic GPCRs | Neurogenic orthostatic hypotension | 61, 62 |
| Albiglutide | GLP-1 glucagon-like receptor agonist | Type 2 diabetes | 63, 64 |
| Vorapaxar | PAR-1 thrombin receptor antagonist | Acute chest pain secondary to coronary artery disease | 65 |
| Olodaterol | β2-Adrenergic receptor agonist | Chronic obstructive pulmonary disease | 66 |
| Suvorexant | OX1/2 orexin receptor antagonist | Insomnia | 67 |
| Naloxegol | MOR-opioid receptor antagonist | Opioid-induced constipation | 68 |
| Dulaglutide | GLP-1 glucagon-like receptor agonist | Type 2 diabetes | 69 |
| Netupitant/palonosetron combination | NK1-neurokinin and 5-HT3 receptor antagonists (note 5-HT3 is a ligand-gated ion channel) | Chemotherapy-induced nausea | 70 |