Clinical data
Other namesRP-5063; RP-5000; Oxaripiprazole[1][2]
Routes of
By mouth
Legal status
Legal status
  • 6-[4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butoxy]-4H-1,4-benzoxazin-3-one
CAS Number
PubChem CID
Chemical and physical data
Molar mass450.36 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)

Brilaroxazine (developmental code names RP-5063 and RP-5000), also known as oxaripiprazole,[1][2] is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder.[3][4][5][6] 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.[7][8] As of May 2015, it is in phase III clinical trials for schizophrenia.[7][8]



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.[6][9] 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.[5][6][9] 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.[9] 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.[9][10]


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


  1. ^ a b Modica MN, Lacivita E, Intagliata S, Salerno L, Romeo G, Pittalà V, Leopoldo M (October 2018). "Structure-Activity Relationships and Therapeutic Potentials of 5-HT7 Receptor Ligands: An Update". J Med Chem. 61 (19): 8475–8503. doi:10.1021/acs.jmedchem.7b01898. PMID 29767995.
  2. ^ a b Jordan, Ann Westcot (14 September 2018). Antidepressants: History, Science, and Issues. ISBN 9781440839276.
  3. ^ Medicines in Development for Mental Health (PDF) (Report). Pharmaceutical Research and Manufacturers of America. 2014. p. 20. Retrieved 2015-05-19.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ a b "About Us". Reviva Pharmaceuticals. Retrieved 2015-05-19.
  8. ^ a b "Product Pipeline". Reviva Pharmaceuticals. Retrieved 2015-05-19.
  9. ^ 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.((cite web)): CS1 maint: multiple names: authors list (link)
  10. ^ 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.