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

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

713

RISPERIDONE


INN
RISPERIDONE

(has an active metabolite)

cas 106266-06-2
CLASS

NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF SCHIZOPHRENIA
DOPAMINE ANTAGONISTS
SEROTONIN ANTAGONISTS

ROUTE (list)

ORAL INTRAMUSCULAR SUBCUTANEOUS

ATC code

N05AX08

PK parameters

F 70 PERCENT
Tmax 1 HOUR
VD 97.5 LITER (65 KILOGRAM)
Cl 21 LITER / HOUR
PPB 90 PERCENT
t1/2 3 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER


Target

TARGET 5-HYDROXYTRYPTAMINE 2A RECEPTOR
D(2) DOPAMINE RECEPTOR
ALPHA 1 ADRENERGIC RECEPTOR
ALPHA 2 ADRENERGIC RECEPTOR
H1 HISTAMINIC RECEPTOR

PDB
6C38 (STRUCTURE OF THE D2 DOPAMINE RECEPTOR BOUND TO THE ATYPICAL ANTIPSYCHOTIC DRUG RISPERIDONE)

Ligand code = 8NU (link to the list of PDB complexes)

Download experimental 3D coordinates of 8NU with added hydrogens

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]-2-methyl-6,7,8,9-tetrahydropyrido[2,1-b]pyrimidin-4-one

Formula:
C23H27FN4O2

Calculated chemical properties:

MW 410.49
NB_atoms 30
XLogP 3.59
PSA 58.689
NB_HD 0
NB_HA 6
fsp3 0.52
Lipinski(0=no;1=yes) 1

FDA
NDA 020272 (label) INN (RISPERIDONE) RISPERDAL (JANSSEN PHARMS) APPROVAL= AP YEAR= 1993
NDA 020588 (label) INN (RISPERIDONE) RISPERDAL (JANSSEN PHARMS) APPROVAL= AP YEAR= 1996
NDA 021346 (label) INN (RISPERIDONE) RISPERDAL CONSTA (JANSSEN PHARMS) APPROVAL= AP YEAR= 2003
NDA 021444 (label) INN (RISPERIDONE) RISPERDAL (JANSSEN PHARMS) APPROVAL= AP YEAR= 2003 DISCONTINUED
NDA 077416 (pdf not found) INN (RISPERIDONE) RISPERIDONE (RANBAXY) APPROVAL= TA YEAR= 2006
NDA 076228 (label) INN (RISPERIDONE) RISPERIDONE (HERITAGE PHARMA AVET) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 076288 (pdf not found) INN (RISPERIDONE) RISPERIDONE (NATCO PHARMA USA) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 077769 (pdf not found) INN (RISPERIDONE) RISPERIDONE (HERITAGE PHARMA AVET) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 077953 (pdf not found) INN (RISPERIDONE) RISPERIDONE (APOTEX INC) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 076879 (pdf not found) INN (RISPERIDONE) RISPERIDONE (DR REDDYS LABS LTD) APPROVAL= AP YEAR= 2008
NDA 077860 (pdf not found) INN (RISPERIDONE) RISPERIDONE (WATSON LABS) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 078040 (pdf not found) INN (RISPERIDONE) RISPERIDONE (ZYDUS PHARMS USA INC) APPROVAL= AP YEAR= 2008
NDA 078269 (pdf not found) INN (RISPERIDONE) RISPERIDONE (RISING) APPROVAL= AP YEAR= 2008
NDA 078707 (pdf not found) INN (RISPERIDONE) RISPERIDONE (RENATA) APPROVAL= AP YEAR= 2008
NDA 078871 (pdf not found) INN (RISPERIDONE) RISPERIDONE (NOVITIUM PHARMA) APPROVAL= AP YEAR= 2008
NDA 079088 (pdf not found) INN (RISPERIDONE) RISPERIDONE (TORRENT PHARMS) APPROVAL= AP YEAR= 2008
NDA 076440 (pdf not found) INN (RISPERIDONE) RISPERIDONE (ANI PHARMS) APPROVAL= AP YEAR= 2009
NDA 076904 (pdf not found) INN (RISPERIDONE) RISPERIDONE (HIKMA) APPROVAL= AP YEAR= 2009 DISCONTINUED
NDA 077328 (label) INN (RISPERIDONE) RISPERIDONE (SENORES PHARMS) APPROVAL= AP YEAR= 2009
NDA 077494 (pdf not found) INN (RISPERIDONE) RISPERIDONE (PH HEALTH) APPROVAL= AP YEAR= 2009
NDA 077719 (pdf not found) INN (RISPERIDONE) RISPERIDONE (PHARM ASSOC) APPROVAL= AP YEAR= 2009 DISCONTINUED
NDA 078071 (pdf not found) INN (RISPERIDONE) RISPERIDONE (AMNEAL) APPROVAL= AP YEAR= 2009
NDA 078116 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SANDOZ) APPROVAL= AP YEAR= 2009
NDA 078187 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SYNTHON PHARMS) APPROVAL= AP YEAR= 2009 DISCONTINUED
NDA 078452 (pdf not found) INN (RISPERIDONE) RISPERIDONE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2009
NDA 078516 (pdf not found) INN (RISPERIDONE) RISPERIDONE (ZYDUS PHARMS USA) APPROVAL= AP YEAR= 2009
NDA 078528 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SANDOZ) APPROVAL= AP YEAR= 2009
NDA 078740 (pdf not found) INN (RISPERIDONE) RISPERIDONE (WEST WARD PHARMS) APPROVAL= AP YEAR= 2009 DISCONTINUED
NDA 078744 (pdf not found) INN (RISPERIDONE) RISPERIDONE (WOCKHARDT BIO AG) APPROVAL= AP YEAR= 2009 DISCONTINUED
NDA 078828 (pdf not found) INN (RISPERIDONE) RISPERIDONE (JUBILANT CADISTA) APPROVAL= AP YEAR= 2009
NDA 078909 (pdf not found) INN (RISPERIDONE) RISPERIDONE (APOZEAL PHARMS) APPROVAL= AP YEAR= 2009
NDA 076797 (pdf not found) INN (RISPERIDONE) RISPERIDONE (PRECISION DOSE) APPROVAL= AP YEAR= 2010 DISCONTINUED
NDA 077542 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2010
NDA 077784 (pdf not found) INN (RISPERIDONE) RISPERIDONE (RATIOPHARM) APPROVAL= AP YEAR= 2010 DISCONTINUED
NDA 078474 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2010
NDA 079158 (pdf not found) INN (RISPERIDONE) RISPERIDONE (LANNETT CO INC) APPROVAL= AP YEAR= 2010 DISCONTINUED
NDA 076996 (pdf not found) INN (RISPERIDONE) RISPERIDONE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 077543 (pdf not found) INN (RISPERIDONE) RISPERIDONE (CHARTWELL MOLECULAR) APPROVAL= AP YEAR= 2011
NDA 090347 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SUN PHARMA CANADA) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 091384 (pdf not found) INN (RISPERIDONE) RISPERIDONE (AMNEAL PHARMS) APPROVAL= AP YEAR= 2011
NDA 091537 (pdf not found) INN (RISPERIDONE) RISPERIDONE (NATCO PHARMA USA) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 077493 (pdf not found) INN (RISPERIDONE) RISPERIDONE (PRINSTON INC) APPROVAL= AP YEAR= 2011
NDA 090839 (pdf not found) INN (RISPERIDONE) RISPERIDONE (JUBILANT GENERICS) APPROVAL= AP YEAR= 2011
NDA 201003 (pdf not found) INN (RISPERIDONE) RISPERIDONE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2011
NDA 076908 (pdf not found) INN (RISPERIDONE) RISPERIDONE (CHARTWELL RX) APPROVAL= AP YEAR= 2012 DISCONTINUED
NDA 079059 (pdf not found) INN (RISPERIDONE) RISPERIDONE (TRIS PHARMA INC) APPROVAL= AP YEAR= 2012
NDA 078464 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 078036 (pdf not found) INN (RISPERIDONE) RISPERIDONE (SUN PHARM INDS INC) APPROVAL= AP YEAR= 2014 DISCONTINUED
NDA 202386 (pdf not found) INN (RISPERIDONE) RISPERIDONE (CHARTWELL MOLECULAR) APPROVAL= AP YEAR= 2015
NDA 210655 (label) INN (RISPERIDONE) PERSERIS KIT (INDIVIOR) APPROVAL= AP YEAR= 2018 DISCONTINUED
NDA 212849 (label) INN (RISPERIDONE) RYKINDO (SHANDONG LUYE) APPROVAL= AP YEAR= 2023
NDA 213586 (label) INN (RISPERIDONE) UZEDY (TEVA) APPROVAL= AP YEAR= 2023
NDA 214068 (pdf not found) INN (RISPERIDONE) RISPERIDONE (TEVA PHARMS USA INC) APPROVAL= AP YEAR= 2023
NDA 214835 (label) INN (RISPERIDONE) RISVAN (LABS FARMS ROVI SA) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 205104 (pdf not found) INN (RISPERIDONE) RISPERIDONE (IPCA LABS LTD) APPROVAL= AP YEAR= 2024
NDA 211220 (pdf not found) INN (RISPERIDONE) RISPERIDONE (NANOMI) APPROVAL= AP YEAR= 2025
NDA 218586 (pdf not found) INN (RISPERIDONE) RISPERIDONE (AMNEAL) APPROVAL= AP YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1487

PALIPERIDONE PALMITATE


INN
PALIPERIDONE PALMITATE

(has an active metabolite)

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

1488

PALIPERIDONE PALMITATE


INN
PALIPERIDONE PALMITATE

(has an active metabolite)

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 82.564
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