Drug target · DRD2

D2

Dopamine D2 receptor

11 compounds in the CNS pipeline act on D2.

Compounds targeting D2

CompoundActionAffinityLead programDeveloper
BrexpiprazoleprimarySmall moleculePartial agonistKi 0.3 nMFiled (NDA)Post-traumatic stress disorderOtsuka Pharmaceutical Co., Ltd.
Olanzapine extended-release injectable suspension (TEV-'749)primarySmall moleculeAntagonistFiled (NDA)SchizophreniaTeva Pharmaceutical Industries Ltd.
Brilaroxazine (RP5063)primarySmall moleculePartial agonistKi 0.37 nMPhase 3SchizophreniaReviva Pharmaceuticals Holdings, Inc.
LB-102 (N-methylamisulpride)primarySmall moleculeAntagonistKi 0.8 nMPhase 3SchizophreniaLB Pharmaceuticals Inc.
LYBALVI (olanzapine/samidorphan)primarySmall moleculeAntagonistKi 11 nMPhase 3SchizophreniaAlkermes plc
ENX-104primarySmall moleculeAntagonistPhase 1Major depressive disorderEngrail Therapeutics, Inc.
Lumateperone (ITI-007)Small moleculeAntagonistKi 32 nMApprovedSchizophreniaIntra-Cellular Therapies, Inc.
Iloperidone LAISmall moleculeAntagonistKi 6.3 nMPhase 3SchizophreniaVanda Pharmaceuticals Inc.
Milsaperidone (VHX-896)Small moleculeAntagonistKi 15.8 nMPhase 3Major depressive disorderVanda Pharmaceuticals Inc.
ALTO-207Small moleculeAgonistPhase 2Treatment-resistant depressionAlto Neuroscience, Inc.
ITI-1284 (deulumateperone)Small moleculeAntagonistPhase 2Alzheimer's diseaseIntra-Cellular Therapies, Inc.