Brexpiprazole: First Global Approval.

Article Details

Citation

Greig SL

Brexpiprazole: First Global Approval.

Drugs. 2015 Sep;75(14):1687-97. doi: 10.1007/s40265-015-0462-2.

PubMed ID
26310190 [ View in PubMed
]
Abstract

Brexpiprazole (Rexulti(R)) is an atypical antipsychotic that has been developed by Otsuka Pharmaceutical Co. Ltd and H. Lundbeck A/S as an oral treatment for several psychiatric disorders. Brexpiprazole is a novel serotonin-dopamine activity modulator that acts as a partial agonist of serotonin 1A (5-HT1A) and dopamine D2 receptors, as well as a potent antagonist of 5-HT2A receptors and noradrenergic alpha1B and alpha2C receptors. In July 2015, brexpiprazole received its first approval in the USA for use as an adjunctive treatment of major depressive disorder (MDD) and the treatment of schizophrenia. In several countries, brexpiprazole is in development for MDDs, schizophrenia, post-traumatic stress disorder and agitation in patients with dementia of the Alzheimer's type. This article summarizes the milestones in the development of brexpiprazole leading to its first global approval in MDD and schizophrenia.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Brexpiprazole5-hydroxytryptamine receptor 1AProteinHumans
Unknown
Partial agonist
Details
Brexpiprazole5-hydroxytryptamine receptor 2AProteinHumans
Unknown
Antagonist
Details
Brexpiprazole5-hydroxytryptamine receptor 2BProteinHumans
Unknown
Antagonist
Details
Brexpiprazole5-hydroxytryptamine receptor 7ProteinHumans
Unknown
Antagonist
Details
BrexpiprazoleAlpha-1A adrenergic receptorProteinHumans
Unknown
Antagonist
Details
BrexpiprazoleAlpha-1B adrenergic receptorProteinHumans
Unknown
Antagonist
Details
BrexpiprazoleAlpha-2C adrenergic receptorProteinHumans
Unknown
Antagonist
Details
BrexpiprazoleDopamine D2 receptorProteinHumans
Unknown
Partial agonist
Details
BrexpiprazoleHistamine H1 receptorProteinHumans
Unknown
Antagonist
Details
BrexpiprazoleMuscarinic acetylcholine receptor M1ProteinHumans
Unknown
Antagonist
Details
Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
BrexpiprazoleCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BrexpiprazoleCytochrome P450 3A4ProteinHumans
No
Substrate
Details
Drug Reactions
Reaction
Details