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

Stem definition	Drug id	CAS RN
psychotropics, phenylpiperazine derivatives	5014	913611-97-9

Description:

Molecule	Description
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: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: OFP

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

Drug dosage:

Dose	Unit	Route
3	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	54.37 hours	Lombardo F, Berellini G, Obach RS
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
BA (Bioavailability)	1 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
CL (Clearance)	0.34 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	530.32	23.50	134	6518	9012	63473358
Schizoaffective disorder	437.86	23.50	96	6556	3466	63478904
Weight increased	357.22	23.50	260	6392	260532	63221838
Tardive dyskinesia	350.17	23.50	95	6557	8407	63473963
Drug level increased	258.19	23.50	95	6557	22641	63459729
Electrocardiogram QT prolonged	204.13	23.50	107	6545	59423	63422947
Product use in unapproved indication	163.28	23.50	141	6511	178939	63303431
Off label use	125.06	23.50	239	6413	674223	62808147
Restlessness	118.41	23.50	59	6593	29394	63452976
Tremor	118.08	23.50	103	6549	132136	63350234

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	331.48	37.60	85	2707	8024	34946115
Weight increased	120.91	37.60	81	2711	92952	34861187
Tardive dyskinesia	108.49	37.60	33	2759	5757	34948382
Product use in unapproved indication	82.75	37.60	71	2721	117428	34836711
Hallucination, auditory	71.18	37.60	29	2763	11888	34942251
Product administered to patient of inappropriate age	66.97	37.60	20	2772	3271	34950868
Suicidal ideation	66.72	37.60	41	2751	40347	34913792
Restlessness	63.95	37.60	34	2758	25448	34928691
Anxiety	59.78	37.60	55	2737	99373	34854766
Psychotic disorder	59.60	37.60	32	2760	24420	34929719

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	281.24	24.59	82	5907	13177	79725222
Tardive dyskinesia	281.12	24.59	78	5911	10493	79727906
Product use in unapproved indication	198.76	24.59	158	5831	250201	79488198
Weight increased	170.36	24.59	151	5838	277235	79461164
Hallucination, auditory	168.41	24.59	62	5927	20631	79717768
Product administered to patient of inappropriate age	107.39	24.59	32	5957	5521	79732878
Tremor	97.03	24.59	89	5900	169994	79568405
Suicidal ideation	96.42	24.59	64	5925	76276	79662123
Restlessness	94.85	24.59	53	5936	46439	79691960
Oculogyric crisis	88.70	24.59	24	5965	2928	79735471

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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

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

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Disease	Relation	SNOMED_ID	DOID
Schizophrenia	indication	58214004	DOID:5419
Major depressive disorder	indication	370143000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.25MG	REXULTI	OTSUKA	N205422	July 10, 2015	RX	TABLET	ORAL	Dec. 27, 2024	NEW PATIENT POPULATION
0.25MG	REXULTI	OTSUKA	N205422	July 10, 2015	RX	TABLET	ORAL	May 10, 2026	TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMER’S DISEASE
0.5MG	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	May 10, 2026	TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMER’S DISEASE
1MG	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	May 10, 2026	TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMER’S DISEASE
2MG	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	May 10, 2026	TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMER’S DISEASE
3MG	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	May 10, 2026	TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMER’S DISEASE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	AGONIST	Ki	9.52	SCIENTIFIC LITERATURE	DRUG LABEL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	AGONIST	Ki	9.92	SCIENTIFIC LITERATURE	DRUG LABEL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.33	SCIENTIFIC LITERATURE	DRUG LABEL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	7.23	SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	7.17	SCIENTIFIC LITERATURE
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN	AGONIST	Ki	6.80	SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.82	SCIENTIFIC LITERATURE
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	IC50	7.54	SCIENTIFIC LITERATURE
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	IC50	6.86	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	8.72	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
016270	NDDF
11978813	PUBCHEM_CID
1658314	RXNORM
234913	MMSL
2J3YBM1K8C	UNII
31120	MMSL
4034625	VUID
4034625	VANDF
716069007	SNOMEDCT_US
7672	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Brexpiprazole	Human Prescription Drug Label	1	27241-204	TABLET	0.25 mg	ORAL	ANDA	32 sections
Brexpiprazole	Human Prescription Drug Label	1	27241-205	TABLET	0.50 mg	ORAL	ANDA	32 sections
Brexpiprazole	Human Prescription Drug Label	1	27241-206	TABLET	1 mg	ORAL	ANDA	32 sections
Brexpiprazole	Human Prescription Drug Label	1	27241-207	TABLET	2 mg	ORAL	ANDA	32 sections
Brexpiprazole	Human Prescription Drug Label	1	27241-208	TABLET	3 mg	ORAL	ANDA	32 sections
Brexpiprazole	Human Prescription Drug Label	1	27241-209	TABLET	4 mg	ORAL	ANDA	32 sections
brexpiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1649	TABLET, FILM COATED	0.25 mg	ORAL	ANDA	29 sections
brexpiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1650	TABLET, FILM COATED	0.50 mg	ORAL	ANDA	29 sections
brexpiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1651	TABLET, FILM COATED	1 mg	ORAL	ANDA	29 sections
brexpiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1652	TABLET, FILM COATED	2 mg	ORAL	ANDA	29 sections

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