e-Drug3D

902

EZETIMIBE


INN
EZETIMIBE

cas 163222-33-1
CLASS

CARDIOVASCULAR
HYPOLIPIDEMIC
ANTICHOLESTEREMIC AGENTS
INHIBITOR OF INTESTINAL CHOLESTEROL ABSORPTION

ROUTE (list)

ORAL

ATC code

C10BA05
C10BA10
C10AX09
C10BA13
C10BA11
C10BA12
C10BA06
C10BA02

PK parameters

Tmax 8 HOUR
PPB 90 PERCENT
t1/2 22 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER


Target

TARGET NIEMANN-PICK C1-LIKE PROTEIN 1 (NPC1L1)

PDB
8AXW (THE STRUCTURE OF MOUSE ASTERC (GRAMD1C) WITH EZETIMIBE)

Ligand code = H56 (link to the list of PDB complexes)

Download experimental 3D coordinates of H56 with added hydrogens

DrugCentral

Niemann-Pick C1-like protein 1 UNIPROT Q9UHC9 NPC1L1

Download SDF file (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one

Formula:
C24H21F2NO3

Calculated chemical properties:

MW 409.42
NB_atoms 30
XLogP 4.89
PSA 59.577
NB_HD 2
NB_HA 4
fsp3 0.21
Lipinski(0=no;1=yes) 1

FDA
NDA 021445 (label) INN (EZETIMIBE) ZETIA (ORGANON) APPROVAL= AP YEAR= 2002 NEWMOLECULARENTITY
NDA 021687 (label) INN (EZETIMIBE ; SIMVASTATIN) VYTORIN (ORGANON) APPROVAL= AP YEAR= 2004
NDA 200153 (label) INN (ATORVASTATIN CALCIUM ; EZETIMIBE) LIPTRUZET (ORGANON) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 078560 (pdf not found) INN (EZETIMIBE) EZETIMIBE (GLENMARK PHARMS LTD) APPROVAL= AP YEAR= 2015
NDA 078724 (pdf not found) INN (EZETIMIBE) EZETIMIBE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2017 DISCONTINUED
NDA 200831 (pdf not found) INN (EZETIMIBE) EZETIMIBE (WATSON LABS INC) APPROVAL= AP YEAR= 2017
NDA 201890 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (ANI PHARMS) APPROVAL= AP YEAR= 2017 DISCONTINUED
NDA 203931 (pdf not found) INN (EZETIMIBE) EZETIMIBE (SANDOZ) APPROVAL= AP YEAR= 2017
NDA 200909 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (DR REDDYS LABS SA) APPROVAL= AP YEAR= 2017
NDA 202968 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (WATSON LABS INC) APPROVAL= AP YEAR= 2017
NDA 204331 (pdf not found) INN (EZETIMIBE) EZETIMIBE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2017
NDA 206084 (pdf not found) INN (ATORVASTATIN CALCIUM ; EZETIMIBE) LYPQOZET (ALTHERA PHARMS) APPROVAL= AP YEAR= 2017
NDA 207311 (pdf not found) INN (EZETIMIBE) EZETIMIBE (OHM LABS INC) APPROVAL= AP YEAR= 2017
NDA 208332 (pdf not found) INN (EZETIMIBE) EZETIMIBE (APOTEX) APPROVAL= AP YEAR= 2017 DISCONTINUED
NDA 208803 (pdf not found) INN (EZETIMIBE) EZETIMIBE (AMNEAL PHARMS CO) APPROVAL= AP YEAR= 2017
NDA 208831 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (AMNEAL PHARMS CO) APPROVAL= AP YEAR= 2017
NDA 209222 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (ALKEM LABS LTD) APPROVAL= AP YEAR= 2017
NDA 209234 (pdf not found) INN (EZETIMIBE) EZETIMIBE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2017
NDA 209838 (pdf not found) INN (EZETIMIBE) EZETIMIBE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2017
NDA 211550 (pdf not found) INN (EZETIMIBE) EZETIMIBE (ACCORD HLTHCARE) APPROVAL= AP YEAR= 2018
NDA 201790 (pdf not found) INN (EZETIMIBE) EZETIMIBE (RISING) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 208699 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (GLENMARK PHARMS LTD) APPROVAL= AP YEAR= 2019
NDA 200082 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (AUROBINDO PHARMA USA) APPROVAL= AP YEAR= 2020
NDA 211617 (label) INN (BEMPEDOIC ACID ; EZETIMIBE) NEXLIZET (ESPERION THERAPS INC) APPROVAL= AP YEAR= 2020
NDA 210673 (pdf not found) INN (EZETIMIBE) EZETIMIBE (SCIEGEN PHARMS INC) APPROVAL= AP YEAR= 2020
NDA 213072 (label) INN (EZETIMIBE ; ROSUVASTATIN CALCIUM) ROSZET (ALTHERA PHARMS) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 210859 (pdf not found) INN (EZETIMIBE) EZETIMIBE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2022
NDA 215693 (pdf not found) INN (EZETIMIBE) EZETIMIBE (ORIENT PHARMA) APPROVAL= AP YEAR= 2022
NDA 211159 (pdf not found) INN (EZETIMIBE) EZETIMIBE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 211663 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (SCIEGEN PHARMS INC) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 209461 (pdf not found) INN (EZETIMIBE ; SIMVASTATIN) EZETIMIBE AND SIMVASTATIN (TORRENT) APPROVAL= AP YEAR= 2025 DISCONTINUED

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL