Table 2.
New drugs (New Molecular Entities, NME) acting via GPCRs that were approved by the FDA in recent years (excluding formulations or pure enantiomers of existing drugs and combinations of previously approved drugs).a
| Drugb (year, structureclass) | Action | Treatment of: |
|---|---|---|
| 2015 | ||
| parathyroid hormone (peptide, MW 9400) | PTH-R agonist | hypocalcemia in patients with hypoparathyroidism |
| brexipiprazole 3bc (phenylpiperazine) | D2 dopamine-R partial agonist | psychosis |
| 2014 | ||
| vorapaxarc8 (decahydro-benzo-isobenzofuran) | PAR1 antagonist | reduction of thrombotic cardiovascular events |
| pasireotide 9 (cyclic peptide, MW 1100) | somatostatin-R agonist | acromegaly |
| suvorexantc10 (benzoxazolyl-diazepan) | orexin-R antagonist | insomnia |
| droxidopa 11 (phenyl-serine) | α-adrenergic-R agonist (precursor of norepinephrine) | neurogenic orthostatic hypotension |
| liraglutide (peptide, MW 3700) | GLP-1-R agonist | chronic weight management |
| albiglutide (peptide-fusion protein, MW 73K) | GLP-1-R agonist | type II diabetes |
| dulaglutide (protein, MW 60K) | GLP-1-R agonist | type II diabetes |
| naloxegol 12 (epoxymorphinan-diol) | µ-opioid-R antagonist | opioid-induced constipation |
| tasimelteon 13 (dihydrobenzofuran) | melatonin-R agonist | non-24-hour sleep–wake disorder in totally blind people |
| olodaterol 14 (benzoxazinone) | β2-adrenergic-R agonist (long acting) | chronic obstructive pulmonary disease |
| 2013 | ||
| macitentan 15 (5-phenylpyrimidine) | endothelin-R antagonist | pulmonary arterial hypertension |
| alogliptin 16 (benzyl-uracil) | DPP IV inhibitor (increases GLP-1 and GIP) | type II diabetes |
| vortioxetine 17 (phenylpiperpazine) | serotonin-R modulator and stimulator | Major Depressive Disorder |
a
a listing of drugs approved by year is at: http://www.centerwatch.com/drug-information/fda-approved-drugs/
b
Structures of small molecules shown in Figure 1.