brexpiprazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
psychotropics, phenylpiperazine derivatives 5014 913611-97-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • brexpiprazole
  • rexulti
  • OPC-34712
  • OPC 34712
an atypical antipsychotic the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors
  • Molecular weight: 433.57
  • Formula: C25H27N3O2S
  • CLOGP: 4.90
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 44.81
  • ALOGS: -5.28
  • ROTB: 7

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
3 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.46 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.34 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 54.37 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 27, 2018 EMA OTSUKA PHARM CO LTD
Jan. 19, 2018 PMDA Otsuka Pharmaceutical Co., Ltd.
July 10, 2015 FDA OTSUKA PHARM CO LTD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Akathisia 414.69 26.22 106 4778 8123 50592117
Weight increased 300.51 26.22 205 4679 201686 50398554
Schizoaffective disorder 262.17 26.22 57 4827 2149 50598091
Off label use 171.07 26.22 218 4666 474208 50126032
Drug level increased 140.27 26.22 57 4827 19211 50581029
Tardive dyskinesia 138.94 26.22 44 4840 7235 50593005
Restlessness 113.07 26.22 53 4831 25120 50575120
Electrocardiogram QT prolonged 104.43 26.22 64 4820 51822 50548418
Product use in unapproved indication 97.14 26.22 84 4800 115735 50484505
Suicidal ideation 88.32 26.22 59 4825 55326 50544914
Mania 81.82 26.22 33 4851 10883 50589357
Inability to afford medication 78.36 26.22 20 4864 1510 50598730
Product administered to patient of inappropriate age 76.47 26.22 22 4862 2608 50597632
Tremor 66.74 26.22 68 4816 114835 50485405
Sinus rhythm 56.62 26.22 13 4871 627 50599613
Drug interaction 47.90 26.22 76 4808 199545 50400695
Extrapyramidal disorder 47.37 26.22 23 4861 11747 50588493
Anger 45.17 26.22 22 4862 11311 50588929
Hallucination, auditory 43.28 26.22 21 4863 10707 50589533
Anxiety 43.11 26.22 68 4816 177538 50422702
Eye movement disorder 38.44 26.22 15 4869 4530 50595710
Depression 38.30 26.22 62 4822 165361 50434879
Wrong technique in product usage process 38.04 26.22 36 4848 55474 50544766
Food craving 37.24 26.22 11 4873 1428 50598812
Collagen-vascular disease 33.65 26.22 6 4878 78 50600162
Oculogyric crisis 32.93 26.22 10 4874 1427 50598813
Insomnia 31.90 26.22 59 4825 174806 50425434
Psychiatric symptom 31.44 26.22 13 4871 4557 50595683
Sedation 31.40 26.22 25 4859 30585 50569655
Adverse event 31.16 26.22 29 4855 43734 50556506
Feeling abnormal 30.34 26.22 48 4836 125444 50474796
Increased appetite 29.67 26.22 15 4869 8346 50591894
Incorrect dose administered 26.86 26.22 28 4856 48386 50551854
Parakeratosis 26.73 26.22 6 4878 261 50599979

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Akathisia 251.60 35.25 64 2009 6678 29565776
Weight increased 118.69 35.25 71 2002 76596 29495858
Off label use 76.70 35.25 99 1974 300701 29271753
Product administered to patient of inappropriate age 73.83 35.25 20 2053 2635 29569819
Tardive dyskinesia 72.57 35.25 23 2050 5235 29567219
Restlessness 60.59 35.25 30 2043 22115 29550339
Anxiety 54.20 35.25 46 2027 85319 29487135
Suicidal ideation 53.09 35.25 32 2041 34684 29537770
Inability to afford medication 49.91 35.25 12 2061 980 29571474
Apathy 49.62 35.25 18 2055 6153 29566301
Psychotic disorder 45.30 35.25 24 2049 20330 29552124
Loss of libido 44.29 35.25 13 2060 2283 29570171
No adverse event 42.87 35.25 22 2051 17456 29554998
Product use in unapproved indication 39.78 35.25 39 2034 86836 29485618
Anger 36.58 35.25 17 2056 10873 29561581
Orthostatic hypertension 35.85 35.25 7 2066 213 29572241

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Akathisia 183.12 28.80 55 4087 11455 64483135
Weight increased 155.49 28.80 120 4022 213228 64281362
Product use in unapproved indication 121.26 28.80 96 4046 176522 64318068
Tardive dyskinesia 116.91 28.80 37 4105 9141 64485449
Product administered to patient of inappropriate age 109.01 28.80 30 4112 4571 64490019
Off label use 105.90 28.80 163 3979 632643 63861947
Restlessness 95.60 28.80 48 4094 39737 64454853
Suicidal ideation 82.49 28.80 52 4090 66490 64428100
Hallucination, auditory 70.70 28.80 30 4112 16909 64477681
Anxiety 62.89 28.80 71 4071 202578 64292012
Inability to afford medication 62.29 28.80 16 4126 1870 64492720
Tremor 60.29 28.80 60 4082 148170 64346420
Apathy 50.57 28.80 21 4121 11211 64483379
Loss of libido 44.81 28.80 13 4129 2391 64492199
Oculogyric crisis 44.11 28.80 13 4129 2525 64492065
Anger 40.75 28.80 20 4122 15721 64478869
Psychotic disorder 37.81 28.80 25 4117 34553 64460037
Collagen-vascular disease 36.94 28.80 6 4136 67 64494523
Suicide attempt 35.00 28.80 32 4110 70975 64423615
Neuroleptic malignant syndrome 34.65 28.80 21 4121 24975 64469615
No adverse event 34.54 28.80 22 4120 28539 64466051
Dissociation 33.66 28.80 11 4131 3000 64491590
Psychiatric symptom 32.59 28.80 13 4129 6260 64488330
Depression 31.40 28.80 48 4094 183243 64311347
Insomnia 31.38 28.80 50 4092 197786 64296804

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX16 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
MeSH PA D015259 Dopamine Agents
MeSH PA D018491 Dopamine Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
FDA EPC N0000175430 Atypical Antipsychotic

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
Major depressive disorder indication 370143000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.14 acidic
pKa2 8.07 Basic
pKa3 0.9 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Dec. 27, 2024 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 9.52 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 1A GPCR AGONIST Ki 9.92 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.33 SCIENTIFIC LITERATURE DRUG LABEL
Beta-1 adrenergic receptor GPCR Ki 7.23 SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor GPCR Ki 7.17 SCIENTIFIC LITERATURE
D(1A) dopamine receptor GPCR AGONIST Ki 6.80 SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor GPCR Ki 7.82 SCIENTIFIC LITERATURE
Sodium-dependent serotonin transporter Transporter INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE
Sodium-dependent noradrenaline transporter Transporter INHIBITOR IC50 6.86 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 8.72 SCIENTIFIC LITERATURE
Alpha-2B adrenergic receptor GPCR Ki 7.77 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 6 GPCR Ki 7.24 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.43 SCIENTIFIC LITERATURE
Alpha-1A adrenergic receptor GPCR Ki 8.42 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1B GPCR Ki 7.50 SCIENTIFIC LITERATURE
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 9.23 SCIENTIFIC LITERATURE
Sodium-dependent dopamine transporter Transporter INHIBITOR IC50 6.03 SCIENTIFIC LITERATURE
D(4) dopamine receptor GPCR AGONIST Ki 8.20 SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.59 SCIENTIFIC LITERATURE
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.77 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 5A GPCR Ki 6.85 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2C GPCR Ki 7.47 SCIENTIFIC LITERATURE
D(3) dopamine receptor GPCR AGONIST Ki 8.96 SCIENTIFIC LITERATURE
Histamine H1 receptor GPCR ANTAGONIST Ki 7.72 SCIENTIFIC LITERATURE
D(2) dopamine receptor GPCR Ki 9.70 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 10.05 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 8.64 CHEMBL

External reference:

IDSource
D10309 KEGG_DRUG
4034625 VUID
N0000191737 NUI
4034625 VANDF
CHEBI:134716 CHEBI
CHEMBL2105760 ChEMBL_ID
C000591922 MESH_SUPPLEMENTAL_RECORD_UI
7672 IUPHAR_LIGAND_ID
9552 INN_ID
DB09128 DRUGBANK_ID
2J3YBM1K8C UNII
11978813 PUBCHEM_CID
1658314 RXNORM
234913 MMSL
31120 MMSL
d08373 MMSL
716069007 SNOMEDCT_US
781292006 SNOMEDCT_US
C3885614 UMLSCUI
016270 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-035 TABLET 0.25 mg ORAL NDA 37 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-036 TABLET 0.50 mg ORAL NDA 37 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-037 TABLET 1 mg ORAL NDA 37 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-038 TABLET 2 mg ORAL NDA 37 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-039 TABLET 3 mg ORAL NDA 37 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-040 TABLET 4 mg ORAL NDA 37 sections