e-Drug3D

1487

PALIPERIDONE PALMITATE

INN
PALIPERIDONE PALMITATE

cas 199739-10-1

CLASS

NERVOUS SYSTEM
ANTIPSYCHOTIC
SCHIZOPHRENIA
BENZISOXAZOLE DERIVATIVES
DOPAMINE D2 RECEPTOR ANTAGONIST
SEROTONIN TYPE 2 (5HT2A) RECEPTOR ANTAGONIST

ROUTE (list)

INTRAMUSCULAR

ATC code

N05AX13

PK parameters

Solubility

VERY SLIGHTLY SOLUBLE IN ETHANOL

Target

TARGET 5-HYDROXYTRYPTAMINE 2A RECEPTOR
D(2) DOPAMINE RECEPTOR
ALPHA1 ADRENERGIC RECEPTOR
ALPHA2 ADRENERGIC RECEPTOR
H1 HISTAMINERGIC RECEPTOR

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file

Hexadecanoic acid, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl ester

Formula:
C39H57FN4O4

Calculated chemical properties:

MW 664.89
NB_atoms 48
XLogP 9.11
PSA 83.131
NB_HD 0
NB_HA 8
fsp3 0.69
Lipinski(0=no;1=yes) 0

FDA
NDA 022264 (label) INN (PALIPERIDONE PALMITATE) INVEGA SUSTENNA (JANSSEN PHARMS) APPROVAL= AP YEAR= 2009
NDA 207946 (label) INN (PALIPERIDONE PALMITATE) INVEGA TRINZA (JANSSEN PHARMS) APPROVAL= AP YEAR= 2015
NDA 211149 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2021 OBSOLETE
NDA 211995 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (TOLMAR) APPROVAL= TA YEAR= 2023
NDA 210397 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (PHARMASCIENCE INC) APPROVAL= TA YEAR= 2024
NDA 216228 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (MYLAN PHARMS INC) APPROVAL= TA YEAR= 2024
NDA 215682 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (MYLAN PHARMACEUTICALS INC A VIATRIS CO) APPROVAL= TA YEAR= 2024
NDA 216352 (label) INN (PALIPERIDONE PALMITATE) ERZOFRI (LUYE INNOMIND PHARMA) APPROVAL= AP YEAR= 2024
NDA 216674 (pdf not found) INN (PALIPERIDONE PALMITATE) PALIPERIDONE PALMITATE (ACCORD HLTHCARE INC) APPROVAL= TA YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

949

PALIPERIDONE

INN
PALIPERIDONE

(is an active metabolite)

cas 144598-75-4

CLASS

NERVOUS SYSTEM
ANTIPSYCHOTIC
SCHIZOPHRENIA
BENZISOXAZOLE DERIVATIVES
DOPAMINE D2 RECEPTOR ANTAGONIST
SEROTONIN TYPE 2 (5HT2A) RECEPTOR ANTAGONIST

ROUTE (list)

ORAL

ATC code

N05AX13

PK parameters

Tmax 3 HOUR
VD 391 LITER
Cl 10.8 LITER / HOUR (EQN)
PPB 74 PERCENT
t1/2 25 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER

Target

TARGET 5-HYDROXYTRYPTAMINE 2A RECEPTOR
D(2) DOPAMINE RECEPTOR
ALPHA1 ADRENERGIC RECEPTOR
ALPHA2 ADRENERGIC RECEPTOR
H1 HISTAMINERGIC RECEPTOR

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file

3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[2,1-b]pyrimidin-4-one

Formula:
C23H27FN4O3

Calculated chemical properties:

MW 426.49
NB_atoms 31
XLogP 3.08
PSA 78.557
NB_HD 1
NB_HA 7
fsp3 0.52
Lipinski(0=no;1=yes) 1

FDA
NDA 021999 (label) INN (PALIPERIDONE) INVEGA (JANSSEN PHARMS) APPROVAL= AP YEAR= 2006
NDA 022043 (label) INN (PALIPERIDONE) INVEGA (JANSSEN LP) APPROVAL= AP YEAR= 2007 NEWAPPLICATION
NDA 202645 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 203802 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (RK PHARMA) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 205618 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (SUN PHARM) APPROVAL= AP YEAR= 2018
NDA 204452 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (INVENTIA) APPROVAL= AP YEAR= 2019
NDA 204707 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (AMNEAL PHARMS) APPROVAL= AP YEAR= 2019
NDA 212807 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (CSPC OUYI) APPROVAL= AP YEAR= 2020
NDA 208643 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (LUPIN) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 216174 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (ASCENT PHARMS INC) APPROVAL= AP YEAR= 2023
NDA 217445 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2024
NDA 218330 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (ALEMBIC) APPROVAL= AP YEAR= 2024
NDA 218514 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2024
NDA 205559 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (DR REDDYS) APPROVAL= AP YEAR= 2025
NDA 218755 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (ESKAYEF) APPROVAL= AP YEAR= 2025
NDA 203279 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (APOTEX) APPROVAL= AP YEAR= 2026 DISCONTINUED
NDA 205402 (pdf not found) INN (PALIPERIDONE) PALIPERIDONE (I3 PHARMS) APPROVAL= AP YEAR= 2026