e-Drug3D

900

ARIPIPRAZOLE


INN
ARIPIPRAZOLE

(is an active metabolite)

cas 129722-12-9
CLASS

NERVOUS SYSTEM
ANTIPSYCHOTICS
TREATMENT OF BIPOLAR I DISORDER (SCHIZOPHRENIA)
D2 DOPAMINE RECEPTOR AGONIST (KI=0.34 NANOMOLAR)
5HT1A AGONIST (KI=1.7 NANOMOLAR)
5HT2A ANTAGONIST (KI=3.4 NANOMOLAR)
ADRENERGIC ALPHA1 RECEPTOR ANTAGONIST
D3 DOPAMINE RECEPTOR PARTIAL AGONIST (KI=0.8 NANOMOLAR)

ROUTE (list)

ORAL INTRAMUSCULAR

ATC code

N05AX12

PK parameters

F 87 PERCENT
Tmax 4 HOUR
VD 404 LITER
Cl 3.2 LITER / HOUR (65 KILOGRAM)
PPB 99 PERCENT
t1/2 75 HOUR

Target

TARGET 5-HYDROXYTRYPTAMINE 1A RECEPTOR
5-HYDROXYTRYPTAMINE 2A RECEPTOR
D2 DOPAMINE RECEPTOR
ADRENERGIC ALPHA1 RECEPTOR

PDB
6A7P (HUMAN SERUM ALBUMIN COMPLEXED WITH ARIPIPRAZOLE)

Ligand code = 9SC (link to the list of PDB complexes)

Download experimental 3D coordinates of 9SC with added hydrogens

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one

Formula:
C23H27Cl2N3O2

Calculated chemical properties:

MW 448.38
NB_atoms 30
XLogP 4.86
PSA 52.374
NB_HD 1
NB_HA 5
fsp3 0.43
Lipinski(0=no;1=yes) 1

FDA
NDA 021436 (label) INN (ARIPIPRAZOLE) ABILIFY (OTSUKA) APPROVAL= AP YEAR= 2002
NDA 021713 (label) INN (ARIPIPRAZOLE) ABILIFY (OTSUKA) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 021729 (label) INN (ARIPIPRAZOLE) ABILIFY (OTSUKA) APPROVAL= AP YEAR= 2006 DISCONTINUED
NDA 021866 (label) INN (ARIPIPRAZOLE) ABILIFY (OTSUKA) APPROVAL= AP YEAR= 2006 DISCONTINUED
NDA 078612 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (BARR LABS INC) APPROVAL= TA YEAR= 2012
NDA 078613 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (BARR LABS INC) APPROVAL= TA YEAR= 2012
NDA 078614 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (SUN PHARMA GLOBAL) APPROVAL= TA YEAR= 2013
NDA 202971 (label) INN (ARIPIPRAZOLE) ABILIFY MAINTENA KIT (OTSUKA PHARM CO LTD) APPROVAL= AP YEAR= 2013
NDA 201519 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (TORRENT) APPROVAL= AP YEAR= 2015
NDA 202101 (label) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ALEMBIC) APPROVAL= AP YEAR= 2015
NDA 202102 (label) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ALEMBIC) APPROVAL= AP YEAR= 2015
NDA 078583 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (APOTEX) APPROVAL= AP YEAR= 2015
NDA 078607 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 078608 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 078708 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 203906 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AMNEAL PHARMS) APPROVAL= AP YEAR= 2015
NDA 204171 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (LANNETT CO INC) APPROVAL= AP YEAR= 2015
NDA 205064 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2015
NDA 203908 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2015
NDA 204094 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (APOTEX) APPROVAL= AP YEAR= 2015
NDA 204838 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AMNEAL PHARMS) APPROVAL= AP YEAR= 2016
NDA 204111 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2016
NDA 206174 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2016
NDA 206251 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ACCORD HLTHCARE) APPROVAL= AP YEAR= 2016
NDA 206383 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (SCIEGEN PHARMS INC) APPROVAL= AP YEAR= 2016
NDA 091279 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AIPING PHARM INC) APPROVAL= AP YEAR= 2017 DISCONTINUED
NDA 202683 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ORBION PHARMS) APPROVAL= AP YEAR= 2017
NDA 202547 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ORBION PHARMS) APPROVAL= AP YEAR= 2017
NDA 205363 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (PRINSTON INC) APPROVAL= AP YEAR= 2017
NDA 207202 (label) INN (ARIPIPRAZOLE) ABILIFY MYCITE KIT (OTSUKA) APPROVAL= AP YEAR= 2017 DISCONTINUED
NDA 090165 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (SQUARE PHARMS) APPROVAL= AP YEAR= 2018
NDA 207240 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (SCIEGEN PHARMS INC) APPROVAL= AP YEAR= 2018
NDA 206240 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (NORVIUM BIOSCIENCE) APPROVAL= AP YEAR= 2018 DISCONTINUED
NDA 208260 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (PHARMTAK INC) APPROVAL= TA YEAR= 2018
NDA 208438 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (PHARMTAK INC) APPROVAL= TA YEAR= 2018
NDA 090472 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 207105 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2019
NDA 210479 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2019
NDA 212870 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (VISTAPHARM LLC) APPROVAL= AP YEAR= 2019
NDA 203025 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (UNICHEM) APPROVAL= AP YEAR= 2021
NDA 215595 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (CHARTWELL RX) APPROVAL= AP YEAR= 2022
NDA 216351 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (RUBICON RESEARCH) APPROVAL= AP YEAR= 2022
NDA 217006 (label) INN (ARIPIPRAZOLE) ABILIFY ASIMTUFII (OTSUKA) APPROVAL= AP YEAR= 2023
NDA 213037 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (SUNSHINE) APPROVAL= AP YEAR= 2023
NDA 216150 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2023
NDA 205589 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (LUPIN) APPROVAL= AP YEAR= 2024
NDA 216608 (pdf not found) INN (ARIPIPRAZOLE) ARIPIPRAZOLE (MYLAN) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 216655 (label) INN (ARIPIPRAZOLE) OPIPZA (XIAMEN LP PHARM CO) APPROVAL= AP YEAR= 2024
NDA 211448 (label) INN (ARIPIPRAZOLE) MEZOFY (CMG PHARM CO LTD) APPROVAL= AP YEAR= 2025 DISCONTINUED

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL