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Brexpiprazole information


Brexpiprazole
Clinical data
Pronunciation/brɛkˈspɪprəzl/ brek-SPIP-rə-zohl
Trade namesRexulti, Rxulti, others
Other namesOPC-34712
AHFS/Drugs.comMonograph
MedlinePlusa615046
License data
  • US DailyMed: Brexpiprazole
Pregnancy
category
  • AU: C[1][2]
Routes of
administration
By mouth
Drug classAtypical antipsychotic
ATC code
  • N05AX16 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[2][4][5][6]
  • BR: Class C1 (Other controlled substances)[7]
  • CA: ℞-only[8][9][10]
  • US: WARNING[3]Rx-only[11]
  • EU: Rx-only[12]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability95% (Tmax = 4 hours)[11]
Protein binding>99%
MetabolismLiver (mainly mediated by CYP3A4 and CYP2D6)
Elimination half-life91 hours (brexpiprazole), 86 hours (major metabolite)
ExcretionFeces (46%), urine (25%)
Identifiers
IUPAC name
  • 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]quinolin-2(1H)-one
CAS Number
  • 913611-97-9
PubChem CID
  • 11978813
DrugBank
  • DB09128
ChemSpider
  • 10152155
UNII
  • 2J3YBM1K8C
KEGG
  • D10309
ChEBI
  • CHEBI:134716
ChEMBL
  • ChEMBL2105760
CompTox Dashboard (EPA)
  • DTXSID40238527 Edit this at Wikidata
ECHA InfoCard100.242.305 Edit this at Wikidata
Chemical and physical data
FormulaC25H27N3O2S
Molar mass433.57 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • O=C5/C=C\c4ccc(OCCCCN3CCN(c1cccc2sccc12)CC3)cc4N5
InChI
  • InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
  • Key:ZKIAIYBUSXZPLP-UHFFFAOYSA-N

Brexpiprazole, sold under the brand name Rexulti among others, is a medication used for the treatment of major depressive disorder, schizophrenia, and agitation associated with dementia due to Alzheimer's disease.[11][13][14] It is an atypical antipsychotic.[11]

The most common side effects include akathisia (a constant urge to move) and weight gain.[12] The most common side effects among people with agitation associated with dementia due to Alzheimer's disease include headache, dizziness, urinary tract infection, nasopharyngitis, and sleep disturbances (both somnolence and insomnia).[13]

Brexpiprazole was developed by Otsuka and Lundbeck, and is considered to be a successor to aripiprazole (Abilify).[15] It was approved for medical use in the United States in July 2015.[16][17] A generic version was approved in August 2022.[18] Brexpiprazole is the first treatment approved by the US Food and Drug Administration (FDA) for agitation associated with dementia due to Alzheimer's disease.[13]

  1. ^ "Brexpiprazole (Rexulti) Use During Pregnancy". Drugs.com. 10 February 2020. Retrieved 18 August 2020.
  2. ^ a b "Rexulti brexpiprazole 4 mg film coated tablets blisters (273224)". Therapeutic Goods Administration (TGA). Retrieved 26 February 2023.
  3. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  4. ^ AusPAR: Brexpiprazole
  5. ^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  6. ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
  7. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  8. ^ "Rexulti Product information". Health Canada. Retrieved 26 February 2023.
  9. ^ Rexulti monograph
  10. ^ "Mental health". Health Canada. 9 May 2018. Retrieved 13 April 2024.
  11. ^ a b c d "Rexulti- brexpiprazole tablet Rexulti- brexpiprazole kit". DailyMed. 21 February 2023. Retrieved 26 February 2023.
  12. ^ a b "Rxulti EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 26 February 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  13. ^ a b c "FDA Approves First Drug to Treat Agitation Symptoms Associated with Dementia due to Alzheimer's Disease". U.S. Food and Drug Administration (FDA) (Press release). 11 May 2023. Retrieved 12 May 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  14. ^ Lee D, Slomkowski M, Hefting N, Chen D, Larsen KG, Kohegyi E, et al. (December 2023). "Brexpiprazole for the Treatment of Agitation in Alzheimer Dementia: A Randomized Clinical Trial". JAMA Neurology. 80 (12): 1307–1316. doi:10.1001/jamaneurol.2023.3810. PMC 10628834. PMID 37930669.
  15. ^ "Otsuka HD places top priority on development of OPC-34712". Chemical Business Newsbase. 3 January 2011. Retrieved 10 February 2012.
  16. ^ "Rexulti (brexpiprazole) Tablets". U.S. Food and Drug Administration (FDA). 10 July 2015. Retrieved 18 August 2020.
  17. ^ "FDA approves new drug to treat schizophrenia and as an add on to an antidepressant to treat ]" (Press release). U.S. Food and Drug Administration (FDA). 13 July 2015. Archived from the original on 15 July 2015. Retrieved 14 July 2015.
  18. ^ "2022 First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Retrieved 30 April 2023.

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