e-Drug3D

1780

BREXPIPRAZOLE


INN
BREXPIPRAZOLE

cas 913611-97-9
CLASS

NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF MAJOR DEPRESSIVE DISORDER OR SCHIZOPHRENIA
COMBINATION OF PARTIAL AGONIST ACTIVITY AT SEROTONIN 5-HT1A (KD = 0.12 NANOMOLAR) AND DOPAMINE D2 (KD = 0.30 NANOMOLAR) AND ANTAGONIST ACTIVITY AT SEROTONIN 5-HT2A RECEPTORS (KD= 0.47 NANOMOLAR)

ROUTE (list)

ORAL

ATC code

N05AX16

PK parameters

F 95 PERCENT
Tmax 4 HOUR
VD 101.4 LITER (65 KILOGRAM)
Cl 1.28 LITER / HOUR (65 KILOGRAM)
PPB 99 PERCENT
t1/2 91 HOUR

Target

TARGET 5-HT1A RECEPTORS
DOPAMINE D2 RECEPTOR
5-HT2A RECEPTOR

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 1A UNIPROT P08908 HTR1A

Download SDF file 2(1H)-Quinolinone, 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-

Formula:
C25H27N3O2S

Calculated chemical properties:

MW 433.57
NB_atoms 31
XLogP 4.72
PSA 52.608
NB_HD 1
NB_HA 5
fsp3 0.32
Lipinski(0=no;1=yes) 1

FDA
NDA 205422 (label) INN (BREXPIPRAZOLE) REXULTI (OTSUKA) APPROVAL= AP YEAR= 2015
NDA 213788 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (ACCORD HLTHCARE INC) APPROVAL= TA YEAR= 2021
NDA 213477 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (ZENARA) APPROVAL= TA YEAR= 2022
NDA 213570 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (SANDOZ) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 213692 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (TEVA PHARMS USA INC) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 213660 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213718 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213782 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213512 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (LUPIN) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213562 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (AMNEAL) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213740 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (MSN PHARMS INC) APPROVAL= TA YEAR= 2023
NDA 213659 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213669 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213758 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (CHARTWELL RX) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 213587 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (PRINSTON PHARMA INC) APPROVAL= TA YEAR= 2024
NDA 213683 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (ALEMBIC) APPROVAL= AP YEAR= 2025
NDA 213731 (pdf not found) INN (BREXPIPRAZOLE) BREXPIPRAZOLE (APOTEX) APPROVAL= AP YEAR= 2025 DISCONTINUED

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL