Drug target · ADRA1A

alpha-1A adrenoceptor

Alpha-1A adrenergic receptor

5 compounds in the CNS pipeline act on alpha-1A adrenoceptor.

Compounds targeting alpha-1A adrenoceptor

CompoundActionAffinityLead programDeveloper
TNX-102 SL (cyclobenzaprine HCl sublingual)Small moleculeAntagonistKi 5.6 nMApprovedFibromyalgiaTonix Pharmaceuticals Holding Corp.
Olanzapine extended-release injectable suspension (TEV-'749)Small moleculeAntagonist—Filed (NDA)SchizophreniaTeva Pharmaceutical Industries Ltd.
Iloperidone LAISmall moleculeAntagonistKi 0.36 nMPhase 3SchizophreniaVanda Pharmaceuticals Inc.
Milsaperidone (VHX-896)Small moleculeAntagonistKi 8.3 nMPhase 3Major depressive disorderVanda Pharmaceuticals Inc.
Roluperidone (MIN-101)Small moleculeAntagonistKi 4.17 nMPhase 3SchizophreniaMinerva Neurosciences, Inc.