Brilaroxazine

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Brilaroxazine
Brilaroxazine.svg
Clinical data
Other namesRP-5063; RP-5000; Oxaripiprazole
Routes of
administration		By mouth
Legal status
Legal status
  • US: Investigational New Drug
Identifiers
IUPAC name
CAS Number
  • 1239729-06-6
    1708960-04-6 (hydrochloride)
PubChem CID
DrugBank
ChemSpider
UNII
Chemical and physical data
FormulaC22H25Cl2N3O3
Molar mass450.36 g·mol−1
3D model (JSmol)
SMILES
InChI

Brilaroxazine, also known by the developmental code names RP-5063 and RP-5000, is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder.[1][2][3][4] 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.[5][6] As of May 2015, it is in phase III clinical trials for schizophrenia.[5][6]

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.[4][7] 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.[3][4][7] 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.[7] 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.[7][8]

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.

See also[]

References[]

  1. ^ Medicines in Development for Mental Health (PDF) (Report). Pharmaceutical Research and Manufacturers of America. 2014. p. 20. Retrieved 2015-05-19.
  2. ^ Köster LS, Carbon M, Correll CU (December 2014). "Emerging drugs for schizophrenia: an update". Expert Opinion on Emerging Drugs. 19 (4): 511–31. doi:10.1517/14728214.2014.958148. PMID 25234340. S2CID 42729570.
  3. ^ Jump up to: a b "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595. S2CID 8513976.
  4. ^ Jump up to: a b c Cantillon M (2014). "Efficacy and Safety of Novel Dopamine Serotonin Stabilizer RP 5063 in Acute Schizophrenia and Schizoaffective Disorder". Schizophrenia Research. 153: S22. doi:10.1016/S0920-9964(14)70070-2. ISSN 0920-9964. S2CID 54373785.
  5. ^ Jump up to: a b "About Us". Reviva Pharmaceuticals. Retrieved 2015-05-19.
  6. ^ Jump up to: a b "Product Pipeline". Reviva Pharmaceuticals. Retrieved 2015-05-19.
  7. ^ Jump up to: a b c d Marc Cantillon, M.D., Mike Li, MS, Sarath Kanekal, Ph.D., DABT, RAC, Robert M.J. Ings, Ph.D., Grace Tung, RAC, Laxminarayan Bhat (2013). "Refresh: A Phase 2 RP5063 Efficacy and Safety in Schizophrenia and Schizoaffective Disorder" (PDF). American Society of Clinical Psychopharmacology. Retrieved 2015-05-19.CS1 maint: multiple names: authors list (link)
  8. ^ Reviva Pharmaceuticals (2012). "Reviva Pharmaceuticals Announces Enrollment of Patients in Phase 2 Clinical Study of RP5063 for the Treatment of Schizophrenia and Schizoaffective Disorder". PipelineReview.

External links[]

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