Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H27N3O2S |
Molecular Weight | 433.566 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C1NC2=C(C=C1)C=CC(OCCCCN3CCN(CC3)C4=CC=CC5=C4C=CS5)=C2
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)
Molecular Formula | C25H27N3O2S |
Molecular Weight | 433.566 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB09128
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
0.12 nM [Ki] | |||
0.47 nM [Ki] | |||
Target ID: CHEMBL217 |
0.3 nM [Ki] | ||
Target ID: CHEMBL234 |
1.1 nM [Ki] | ||
Target ID: CHEMBL1833 |
1.9 nM [Ki] | ||
Target ID: CHEMBL1916 |
0.59 nM [Ki] | ||
Target ID: CHEMBL232 |
0.17 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | REXULTI Approved UseREXULTI 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 Date2015 |
|||
Primary | REXULTI Approved UseREXULTI 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 Date2015 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
165 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3238 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
70.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28750151 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
unknown, unknown |
BREXPIPRAZOLE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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... |
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%) Sources: Page: p. 132Coronary 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%) |
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%) Sources: Page: p. 132Electrocardiogram QT prolonged (1.1%) Akathisia (1.1%) Syncope (1.1%) Tremor (1.1%) Agitation (1.1%) |
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%) Sources: Page: p. 132Vomiting (0.3%) |
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%) Sources: Page: p. 132Ankle fracture (0.3%) Aspartate aminotransferase increased (0.3%) Agitation (0.3%) Hallucination (0.3%) Aggression (0.3%) |
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 |
Sources: Page: p. 118 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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) Comment: lovastatin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/205422Orig1Orig2s000ClinPharmR.pdf#page=11 Page: 11.0 |
|||
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
PubMed
Title | Date | PubMed |
---|---|---|
Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. | 2014 Sep |
|
The preclinical profile of brexpiprazole: what is its clinical relevance for the treatment of psychiatric disorders? | 2015 Oct |
|
Brexpiprazole: First Global Approval. | 2015 Sep |
|
Brexpiprazole for schizophrenia and as adjunct for major depressive disorder: a systematic review of the efficacy and safety profile for this newly approved antipsychotic - what is the number needed to treat, number needed to harm and likelihood to be helped or harmed? | 2015 Sep |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/rexulti.html
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25687838
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
Edited
Sat Dec 16 01:28:09 GMT 2023
by
admin
on
Sat Dec 16 01:28:09 GMT 2023
|
Record UNII |
2J3YBM1K8C
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
N05AX16
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
||
|
NDF-RT |
N0000175430
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
2J3YBM1K8C
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
913611-97-9
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
1658314
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | RxNorm | ||
|
100000141399
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
C166575
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
2J3YBM1K8C
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
5014
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
CHEMBL2105760
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
DTXSID40238527
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
7672
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
m11883
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
11978813
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
Brexpiprazole
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
BREXPIPRAZOLE
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
YY-38
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
9552
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
DB09128
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY | |||
|
SUB91646
Created by
admin on Sat Dec 16 01:28:09 GMT 2023 , Edited by admin on Sat Dec 16 01:28:09 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
METABOLIC ENZYME -> NON-SUBSTRATE | |||
|
METABOLIC ENZYME -> NON-SUBSTRATE | |||
|
TARGET->PARTIAL AGONIST |
BINDING
Ki
|
||
|
METABOLIC ENZYME -> NON-SUBSTRATE | |||
|
TARGET->PARTIAL AGONIST |
Ki
|
||
|
METABOLIC ENZYME -> NON-SUBSTRATE | |||
|
TARGET -> INHIBITOR |
Ki
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
TARGET -> INHIBITOR |
Ki
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE LESS ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT | |||
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT | |||
|
METABOLITE LESS ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT |
MINOR
|
||
|
METABOLITE -> PARENT | |||
|
METABOLITE LESS ACTIVE -> PARENT | |||
|
METABOLITE LESS ACTIVE -> PARENT |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
|
|
|||
Volume of Distribution | PHARMACOKINETIC |
|
|
|||