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Atypical antipsychotic
Brilaroxazine
Другие языки:

Brilaroxazine

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Brilaroxazine
Brilaroxazine.svg
Clinical data
Other names RP-5063; RP-5000; Oxaripiprazole
Routes of
administration		 By mouth
Legal status
Legal status
Identifiers
  • 6-[4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butoxy]-4H-1,4-benzoxazin-3-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
Chemical and physical data
Formula C22H25Cl2N3O3
Molar mass 450.36 g·mol−1
3D model (JSmol)
  • C1CN(CCN1CCCCOC2=CC3=C(C=C2)OCC(=O)N3)C4=C(C(=CC=C4)Cl)Cl
  • InChI=1S/C22H25Cl2N3O3/c23-17-4-3-5-19(22(17)24)27-11-9-26(10-12-27)8-1-2-13-29-16-6-7-20-18(14-16)25-21(28)15-30-20/h3-7,14H,1-2,8-13,15H2,(H,25,28)
  • Key:PMKMNTBZJOXTJW-UHFFFAOYSA-N

Brilaroxazine (developmental code names RP-5063 and RP-5000), also known as oxaripiprazole, is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder. Reviva Pharmaceuticals also intends to investigate brilaroxazine for the treatment of bipolar disorder, major depressive disorder, psychosis/agitation associated with Alzheimer's disease, Parkinson's disease psychosis, attention deficit hyperactivity disorder (ADD/ADHD), and autism. As of August 2022, it is in phase III clinical trials for schizophrenia.

Pharmacology

Pharmacodynamics

Brilaroxazine is described as a so-called "dopamine-serotonin system stabilizer" due to its unique actions on the dopamine and serotonin neurotransmitter systems compared to other antipsychotics. Specifically, it acts as a partial agonist of the D2, D3, and D4 receptors and of the 5-HT1A and 5-HT2A receptors, and as an antagonist of the 5-HT6 and 5-HT7 receptors. Brilaroxazine has high affinity for the D2S, D2L, D3, D4.4, 5-HT1A, 5-HT2A, 5-HT7, and H1 receptors, and moderate affinity for the D1, D5, 5-HT3, 5-HT6 receptors, the serotonin transporter, and the α1B-adrenergic receptor. It lacks significant affinity for the 5-HT1B, 5-HT2C, α2-adrenergic, and muscarinic acetylcholine receptors, as well as for the norepinephrine and dopamine transporters.

Chemistry

Brilaroxazine is identical to aripiprazole in chemical structure except for the replacement of one of the carbon atoms in aripiprazole's quinolinone ring system with an oxygen atom, resulting instead in a benzoxazinone ring system. The drug is also closely related structurally to brexpiprazole and cariprazine.

Recent Developments

In August, 2022, Reviva Pharmaceuticals, the manufacturer of brilaroxazine, announced successful enrollment of approximately one fifth of study participants for a phase III clinical trial of the drug. The study, which includes clinical sites in the United States, Europe and Asia, aims to assess the efficacy of this agent in the treatment of schizophrenia. A letter from the CEO released in January of 2023 noted no major adverse drug effects were observed as of that date and that enrollment was progressing well. An anticipated study completion date in late 2023 is anticipated. If successful commercial availability is anticipated in early 2025.

See also

External links


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