brexpiprazole indications/contra

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: 4.65
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 44.81
  • ALOGS: -5.28
  • ROTB: 7

Drug dosage:

DoseUnitRoute
3 mg O

Approvals:

DateAgencyCompanyOrphan
July 10, 2015 FDA OTSUKA PHARM CO LTD

FDA Adverse Event Reporting System

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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
Off label use 1048.63 49.48 295 1174 53682 3330708
Akathisia 832.47 49.48 144 1325 2519 3381871
Weight increased 688.40 49.48 184 1285 26556 3357834
Restlessness 226.44 49.48 59 1410 7379 3377011
Anxiety 169.05 49.48 71 1398 39558 3344832
Drug administered to patient of inappropriate age 136.05 49.48 28 1441 1224 3383166
Wrong technique in product usage process 135.84 49.48 48 1421 16703 3367687
Mania 117.37 49.48 31 1438 4047 3380343
Tardive dyskinesia 116.64 49.48 28 1441 2483 3381907
Suicidal ideation 111.03 49.48 42 1427 17663 3366727
Inability to afford medication 107.02 49.48 16 1453 98 3384292
Feeling abnormal 106.07 49.48 46 1423 27479 3356911
Depression 95.78 49.48 48 1421 39722 3344668
Tremor 95.40 49.48 43 1426 28101 3356289
Insomnia 91.37 49.48 45 1424 35853 3348537
Extrapyramidal disorder 82.17 49.48 23 1446 3720 3380670
Anger 82.13 49.48 24 1445 4527 3379863
Drug ineffective 69.00 49.48 58 1411 116032 3268358
Product use issue 68.98 49.48 29 1440 15972 3368418
Sedation 67.03 49.48 22 1447 6079 3378311
Irritability 60.90 49.48 24 1445 11192 3373198
Increased appetite 56.84 49.48 15 1454 1941 3382449
Adverse event 56.74 49.48 23 1446 11534 3372856
Rash 53.92 49.48 41 1428 70780 3313610
Agitation 53.90 49.48 26 1443 19680 3364710
Blood glucose increased 51.56 49.48 25 1444 19130 3365260

Pharmacologic Action:

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

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004
Major depressive disorder indication 370143000

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL Sept. 23, 2019 UPDATES TO THE PRODUCT INFORMATION REGARDING MAINTENANCE TREATMENT OF SCHIZOPHRENIA IN ADULTS BASED UPON THE RESULTS FROM STUDY 331-10-232
0.25MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY
0.5MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY
1MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY
2MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY
3MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY
4MG REXULTI OTSUKA PHARM CO LTD N205422 July 10, 2015 RX TABLET ORAL July 10, 2020 NEW CHEMICAL ENTITY

Bioactivity Summary:

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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
5-hydroxytryptamine receptor 2C GPCR Ki 7.47 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 5A GPCR Ki 6.85 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 6 GPCR Ki 7.24 SCIENTIFIC LITERATURE
Alpha-1A adrenergic receptor GPCR Ki 8.42 SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor GPCR Ki 7.82 SCIENTIFIC LITERATURE
Alpha-2B adrenergic receptor GPCR Ki 7.77 SCIENTIFIC LITERATURE
Beta-1 adrenergic receptor GPCR Ki 7.23 SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor GPCR Ki 7.17 SCIENTIFIC LITERATURE
Sodium-dependent serotonin transporter Transporter INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE
Sodium-dependent noradrenaline transporter Transporter INHIBITOR IC50 6.86 SCIENTIFIC LITERATURE
Sodium-dependent dopamine transporter Transporter INHIBITOR IC50 6.02 SCIENTIFIC LITERATURE
D(3) dopamine receptor GPCR AGONIST Ki 8.96 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 8.72 SCIENTIFIC LITERATURE
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.77 SCIENTIFIC LITERATURE
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 9.23 SCIENTIFIC LITERATURE
Histamine H1 receptor GPCR ANTAGONIST Ki 7.72 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.43 SCIENTIFIC LITERATURE
D(1A) dopamine receptor GPCR AGONIST Ki 6.80 SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.59 SCIENTIFIC LITERATURE
D(4) dopamine receptor GPCR AGONIST Ki 8.20 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1B GPCR Ki 7.49 SCIENTIFIC LITERATURE

External reference:

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

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-035 TABLET 0.25 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-036 TABLET 0.50 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-037 TABLET 1 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-038 TABLET 2 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-039 TABLET 3 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 59148-040 TABLET 4 mg ORAL NDA 21 sections
REXULTI HUMAN PRESCRIPTION DRUG LABEL 1 69189-0642 TABLET 1 mg ORAL NDA 21 sections