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Details

Stereochemistry ACHIRAL
Molecular Formula C25H27N3O2S
Molecular Weight 433.5678
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BREXPIPRAZOLE

SMILES

C(CCOc1ccc2ccc(nc2c1)O)CN3CCN(CC3)c4cccc5c4ccs5

InChI

InChIKey=ZKIAIYBUSXZPLP-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Molecular Formula C25H27N3O2S
Molecular Weight 433.5678
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB09128

Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for major depressive disorder (MDD). Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).Brexpiprazole is sold under the brand name Rexulti. Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
REXULTI

Approved Use

REXULTI is an atypical antipsychotic indicated for: • Use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) • Treatment of schizophrenia

Launch Date

1.43648634E12
Primary
REXULTI

Approved Use

REXULTI is an atypical antipsychotic indicated for: • Use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) • Treatment of schizophrenia

Launch Date

1.43648634E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
165 ng/mL
4 mg 1 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
206 ng/mL
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
29.3 ng/mL
1 mg 1 times / day multiple, oral
dose: 1 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3238 ng × h/mL
4 mg 1 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
3738 ng × h/mL
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
537 ng × h/mL
1 mg 1 times / day multiple, oral
dose: 1 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
70.6 h
4 mg 1 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
51.9 h
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
91.9 h
1 mg 1 times / day multiple, oral
dose: 1 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BREXPIPRAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
unknown, unknown
BREXPIPRAZOLE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, 18-65 years
n = 477
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 18-65 years
Sex: M+F
Population Size: 477
Sources:
Other AEs: Somnolence, Akathisia...
Other AEs:
Somnolence
Akathisia
Weight gain
Sources:
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Disc. AE: Rash, Coronary artery disease...
AEs leading to
discontinuation/dose reduction:
Rash (0.3%)
Coronary artery disease (0.1%)
Gastrooesophageal reflux disease (0.1%)
Irritability (0.1%)
Oedema peripheral (0.1%)
Hepatic enzyme increased (0.4%)
Blood creatine phosphokinase increased (0.1%)
Blood triglycerides increased (0.1%)
Hypoglycaemia (0.1%)
Rhabdomyolysis (0.2%)
Convulsion (0.1%)
Dizziness (0.1%)
Psychomotor hyperactivity (0.1%)
Agitation (0.1%)
Hallucination (0.1%)
Hostility (0.1%)
Sources: Page: p. 132
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Disc. AE: Irritability, Electrocardiogram QT prolonged...
AEs leading to
discontinuation/dose reduction:
Irritability (1.1%)
Electrocardiogram QT prolonged (1.1%)
Akathisia (1.1%)
Syncope (1.1%)
Tremor (1.1%)
Agitation (1.1%)
Sources: Page: p. 132
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.7 years
n = 341
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.7 years
Sex: M+F
Population Size: 341
Sources: Page: p. 132
Disc. AE: Anaemia folate deficiency...
AEs leading to
discontinuation/dose reduction:
Anaemia folate deficiency (0.3%)
Sources: Page: p. 132
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 182
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 182
Sources: Page: p. 132
Disc. AE: Acute myocardial infarction, Vomiting...
AEs leading to
discontinuation/dose reduction:
Acute myocardial infarction (0.3%)
Vomiting (0.3%)
Sources: Page: p. 132
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Disc. AE: Irritability, Ankle fracture...
AEs leading to
discontinuation/dose reduction:
Irritability (0.3%)
Ankle fracture (0.3%)
Aspartate aminotransferase increased (0.3%)
Agitation (0.3%)
Hallucination (0.3%)
Aggression (0.3%)
Sources: Page: p. 132
5 mg 1 times / day steady, oral
Highest studied dose
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources: Page: p. 118
unhealthy, 48 years
n = 1
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 48 years
Sex: F
Population Size: 1
Sources: Page: p. 118
AEs

AEs

AESignificanceDosePopulation
Akathisia
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, 18-65 years
n = 477
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 18-65 years
Sex: M+F
Population Size: 477
Sources:
Somnolence
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, 18-65 years
n = 477
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 18-65 years
Sex: M+F
Population Size: 477
Sources:
Weight gain
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, 18-65 years
n = 477
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 18-65 years
Sex: M+F
Population Size: 477
Sources:
Agitation 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Blood creatine phosphokinase increased 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Blood triglycerides increased 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Convulsion 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Coronary artery disease 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Dizziness 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Gastrooesophageal reflux disease 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Hallucination 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Hostility 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Hypoglycaemia 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Irritability 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Oedema peripheral 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Psychomotor hyperactivity 0.1%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Rhabdomyolysis 0.2%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Rash 0.3%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Hepatic enzyme increased 0.4%
Disc. AE
4 mg 1 times / day steady, oral (max)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 38.8 years
n = 822
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8 years
Sex: M+F
Population Size: 822
Sources: Page: p. 132
Agitation 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Akathisia 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Electrocardiogram QT prolonged 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Irritability 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Syncope 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Tremor 1.1%
Disc. AE
4 mg 1 times / day steady, oral (min)
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.5 years
n = 93
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.5 years
Sex: M+F
Population Size: 93
Sources: Page: p. 132
Anaemia folate deficiency 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 39.7 years
n = 341
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 39.7 years
Sex: M+F
Population Size: 341
Sources: Page: p. 132
Acute myocardial infarction 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 182
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 182
Sources: Page: p. 132
Vomiting 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 182
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 182
Sources: Page: p. 132
Aggression 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Agitation 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Ankle fracture 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Aspartate aminotransferase increased 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Hallucination 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
Irritability 0.3%
Disc. AE
2 mg 1 times / day steady, oral (max)
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources: Page: p. 132
unhealthy, 43.9 years
n = 949
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 43.9 years
Sex: M+F
Population Size: 949
Sources: Page: p. 132
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
weak
weak
yes [IC50 0.16 uM]
yes [IC50 1.16 uM]
yes [IC50 1.6 uM]
yes [IC50 11.4 uM]
yes [IC50 13 uM]
yes [IC50 13.44 uM]
yes [IC50 15.3 uM]
yes [IC50 22.23 uM]
yes [IC50 25.8 uM]
yes [IC50 29.88 uM]
no (co-administration study)
yes [IC50 3.04 uM]
yes [IC50 39.82 uM]
yes [IC50 4.27 uM]
yes [IC50 6.3 uM]
yes [IC50 6.5 uM]
yes [IC50 7.84 uM]
yes [IC50 8.39 uM]
yes [IC50 9.13 uM]
yes [Ki 5.01 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
weak
yes
yes
yes
yes
yes
yes
yes (pharmacogenomic study)
Comment: In CYP2D6 PM subjects, ultra-rapid and intermediate CYP2D6 metabolizer subjects, CL/F was estimated to be -32%, +18% and -20% than the value estimated for CYP2D6 EM subjects, corresponding to +47%, -21% and +25% change in AUC in these subjects, respectively.
Page: 141.0
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
The preclinical profile of brexpiprazole: what is its clinical relevance for the treatment of psychiatric disorders?
2015 Oct
Patents

Sample Use Guides

In Vivo Use Guide
Treatment of Schizophrenia The recommended starting dosage for REXULTI (Brexpiprazole) is 1 mg once daily on Days 1 to 4, taken orally with or without food The recommended target REXULTI dosage is 2 mg to 4 mg once daily. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 4 mg.
Route of Administration: Oral
Brexpiprazole (1.0 uM) increased the number of cells with neurites in PC12 cells. Treatment with brexpiprazole (0.001, 0.01, 0.1 or 1.0 uM) in conjunction with NGF (2.5 ng/ml) increased the number of cells with neurites, in a concentration-dependent manner.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:39:59 UTC 2021
Edited
by admin
on Fri Jun 25 21:39:59 UTC 2021
Record UNII
2J3YBM1K8C
Record Status Validated (UNII)
Record Version
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Name Type Language
BREXPIPRAZOLE
DASH   INN   USAN   WHO-DD  
INN   USAN  
Official Name English
BREXPIPRAZOLE [WHO-DD]
Common Name English
OPC-34712
Code English
BREXPIPRAZOLE [MI]
Common Name English
BREXPIPRAZOLE [INN]
Common Name English
BREXPIPRAZOLE [USAN]
Common Name English
BREXPIPRAZOLE [JAN]
Common Name English
REXULTI
Brand Name English
BREXPIPRAZOLE [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
WHO-ATC N05AX16
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
NDF-RT N0000175430
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
Code System Code Type Description
CAS
913611-97-9
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
RXCUI
1658314
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY RxNorm
NCI_THESAURUS
C166575
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
FDA UNII
2J3YBM1K8C
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
DRUG CENTRAL
5014
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL2105760
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
EPA CompTox
913611-97-9
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
IUPHAR
7672
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
MERCK INDEX
M11883
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
PUBCHEM
11978813
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
LACTMED
Brexpiprazole
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
WIKIPEDIA
BREXPIPRAZOLE
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
INN
9552
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
DRUG BANK
DB09128
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
EVMPD
SUB91646
Created by admin on Fri Jun 25 21:39:59 UTC 2021 , Edited by admin on Fri Jun 25 21:39:59 UTC 2021
PRIMARY
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