Table 1.
Top selling pharmaceuticals that act, directly or indirectly, via GPCRs (Peak Sales Year, as of 2013).a
| Drugb (structure class) | Action | Treatment of: | Peak year sales (~ billion $) |
|---|---|---|---|
| clopidogrel 1 (thienopyridine) | P2Y12R antagonist (prodrug) | thrombosis | 9 |
| salmeterol 2 (phenylethanolamine) | β2 adrenergic-R agonist | asthma | 8 |
| aripiprazole 3a (phenylpiperazine) | D2 dopamine-R partial agonist | psychosis | 7 |
| quetiapine 4 (dibenzothiazepine- piperazine) | antagonist, biogenic amine Rs | psychosis | 6 |
| valsartan 5 (tetrazolyl-biphenyl) | AT1R antagonist | high blood pressure, congestive heart failure | 6 |
| montelukast 6 (phenylvinyl- quinoline) | CysLT2R antagonist | asthma, allergies | 6 |
| olanzapine 7 (piperazinyl- benzodiazepine) | 5HT2 serotonin-R and D2 dopamine-R antagonist | psychosis | 5 |
a
source of sales information: http://pharmamkting.blogspot.com/2013/01/lipitor-plavix-last-of-small-molecule.html
b
Structures shown in Figure 1.