Ezetimibe

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H21F2NO3
Molecular Weight	409.4252
Optical Activity	( - )
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@@H](CC[C@@H]1[C@H](N(C1=O)C2=CC=C(F)C=C2)C3=CC=C(O)C=C3)C4=CC=C(F)C=C4

InChI

InChIKey=OLNTVTPDXPETLC-XPWALMASSA-N

InChI=1S/C24H21F2NO3/c25-17-5-1-15(2-6-17)22(29)14-13-21-23(16-3-11-20(28)12-4-16)27(24(21)30)19-9-7-18(26)8-10-19/h1-12,21-23,28-29H,13-14H2/t21-,22+,23-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C24H21F2NO3
Molecular Weight	409.4252
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.drugbank.ca/drugs/DB00973
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/ezetimibe.html

Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes. Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Niemann-Pick C1-like protein 1 2 Target ID: CHEMBL2027 Sources: http://www.drugbank.ca/drugs/DB00973	Inhibitor 8504
Acyl coenzyme A:cholesterol acyltransferase 1 15 Target ID: CHEMBL2782 Sources: http://www.drugbank.ca/drugs/DB00973	Inhibitor 8504
Niemann-Pick C1-like protein 1 2 Target ID: CHEMBL5161 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18063367	Inhibitor 8504	200.0 nM [Ki]
Leishmania amazonensis 8 Target ID: CHEMBL612877 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27600041	Inhibitor 8504	30.0 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Hyperlipidemia 82 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021445Orig1s037lbl.pdf	Primary	Approved 8583	ZETIA Approved Use Ezetimibe, administered alone, is indicated as adjunctive therapy to diet for the reduction of elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia. Launch Date 2002
Homozygous familial hypercholesterolemia 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021445Orig1s037lbl.pdf	Primary	Approved 8583	ZETIA Approved Use Homozygous Familial Hypercholesterolemia (HoFH) The combination of Ezetimibe and atorvastatin or simvastatin is indicated for the reduction of elevated total-C and LDL-C levels in patients with HoFH, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable. Launch Date 2002
Homozygous familial sitosterolemia 1 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021445Orig1s037lbl.pdf	Primary	Approved 8583	ZETIA Approved Use Ezetimibe is indicated as adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia. Launch Date 2002

C_max

Value	Dose	Analyte	Population
3.4 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21445lbl.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	EZETIMIBE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: FASTED
5.2 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/15871634	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EZETIMIBE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.4 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/15871634	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EZETIMIBE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
86 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/15871634	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		EZETIMIBE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
92 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/15871634	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		EZETIMIBE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
10% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21445lbl.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		EZETIMIBE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/33644733	unhealthy, 57 years Health Status: unhealthy Age Group: 57 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/33644733	Disc. AE: Liver injury... AEs leading to discontinuation/dose reduction: Liver injury Sources: https://pubmed.ncbi.nlm.nih.gov/33644733
10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00867165	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT00867165	Other AEs: Epilepsy congenital, Appendicitis... Other AEs: Epilepsy congenital (serious, 1 patient) Appendicitis (serious, 1 patient) Upper respiratory tract infection (below serious, 7 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00867165
50 mg 1 times / day multiple, oral Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21445lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21445lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21445lbl.pdf
10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01611883	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01611883	Other AEs: Cataract, Abdominal pain upper... Other AEs: Cataract (serious, 1 patient) Abdominal pain upper (serious, 1 patient) Type 2 diabetes mellitus (below serious, 7 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01611883

AEs

AE	Significance	Dose	Population
Liver injury	Disc. AE	10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/33644733	unhealthy, 57 years Health Status: unhealthy Age Group: 57 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/33644733
Upper respiratory tract infection	below serious, 7 patients	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00867165	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT00867165
Appendicitis	serious, 1 patient	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00867165	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT00867165
Epilepsy congenital	serious, 1 patient	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00867165	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT00867165
Type 2 diabetes mellitus	below serious, 7 patients	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01611883	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01611883
Abdominal pain upper	serious, 1 patient	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01611883	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01611883
Cataract	serious, 1 patient	10 mg 1 times / day steady, oral Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01611883	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01611883

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087		inhibitor 2507 inducer 109	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 227 P-gp 1741 CYP1A2 2153 CYP2C8/9 42 BCRP 910 OATP1B1 1079	CYP 303 P-gp 2052 UGT1A1 479 UGT1A3 470 UGT2B15 236 MRP2 252	CYP1A2 832 CYP2C8/9 1

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP2C8/9 42	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP2C8/9 42	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0	not significant	unlikely (co-administration study) Comment: administered using cocktail approach: caffeine, tolbutamide, dextromethorphan, IV midazolam, and dapsone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=19 Page: 19.0
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes [IC50 0.25 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/dmd/44/3/398.full.pdf#page=11 Page: 11.0	yes [IC50 2.2 uM]	unlikely Comment: page 8: R-value extrapolation indicate potential for DDI as unlikely Sources: https://dmd.aspetjournals.org/content/dmd/44/3/398.full.pdf#page=11 Page: 11.0
BCRP 985	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/dmd/44/3/398.full.pdf#page=11 Page: 11.0	yes [IC50 2.9 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes [IC50 24 uM]

Drug as victim

Target	Modality	Activity
CYP 303	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	no
MRP2 252	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/17828742/	yes
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes
UGT2B15 236	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21445_Zetia_biopharmr_P1.pdf#page=18 Page: 18.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ema.europa.eu/en/documents/assessment-report/nustendi-epar-public-assessment-report_en.pdf#page=31 Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:49040	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:49040
ChemicalBook	CB7380787	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7380787
eMolecules	2736798	https://www.emolecules.com/cgi-bin/more?vid=2736798
MolPort	MolPort-005-938-627	https://www.molport.com/shop/molecule-link/MolPort-005-938-627
Selleck Chemicals	Ezetimibe(Zetia)	http://www.selleckchem.com/products/Ezetimibe(Zetia).html
ZINC	ZINC000003810860	http://zinc15.docking.org/substances/ZINC000003810860

PubMed

Title	Date	PubMed
Ezetimibe added to ongoing statin therapy reduced LDL cholesterol in primary hypercholesterolemia.	2003-07-05	12841712
Perspectives in cholesterol-lowering therapy: the role of ezetimibe, a new selective inhibitor of intestinal cholesterol absorption.	2003-07-01	12835406
Evaluation of the efficacy, safety, and tolerability of ezetimibe in primary hypercholesterolaemia: a pooled analysis from two controlled phase III clinical studies.	2003-06	12846338
Sterol absorption by the small intestine.	2003-06	12840653
Cholesterol absorption inhibitors: defining new options in lipid management.	2003-06	12839042
Ezetimibe for management of hypercholesterolemia.	2003-06	12773075
Combination lipid-lowering therapy in diabetes.	2003-06	12762976
[Coronary disease prevention: only the inhibition of inflammation is important. Why lower lipids, too?].	2003-05-22	12845862
New lipid-lowering combo proves successful.	2003-05-20	12756195
Effect of ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial.	2003-05-20	12719279
[Controlling LDL cholesterol from 2 sides. "I have never seen such low LDL values"].	2003-05-15	12822234
Gateways to clinical trials.	2003-05	12808477
Three new drugs for hyperlipidemia.	2003-05	12802842
52nd Annual Scientific Session of the American College of Cardiology, Chicago, March 30-April 2, 2003.	2003-05	12800468
Statins, super-statins and cholesterol absorption inhibitors.	2003-05	12789600
Treating dyslipidemic patients with lipid-modifying and combination therapies.	2003-05	12741437
Familial hypercholesterolemia--improving treatment and meeting guidelines.	2003-05	12727001
Synthesis of a biotin-tagged photoaffinity probe of 2-azetidinone cholesterol absorption inhibitors.	2003-04-17	12659749
Zetia (ezetimibe).	2003-04-03	12671344
Ezetimibe.	2003-04	12743640
Ezetimibe potently inhibits cholesterol absorption but does not affect acute hepatic or intestinal cholesterol synthesis in rats.	2003-04	12721101
Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia.	2003-04	12713767
Efficacy and safety of ezetimibe coadministered with pravastatin in patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial.	2003-04	12713766
Combined lipid lowering drug therapy for the effective treatment of hypercholesterolaemia.	2003-04	12713763
New drug joins cholesterol-fighting arsenal.	2003-04	12660603
Three new drugs for hyperlipidemia.	2003-03-03	12612501
What future for combination therapies?	2003-03	12793597
New cholesterol-lowering drug makes its mark.	2003-03	12703463
New lipid-modifying therapies.	2003-03	12605558
Efficacy and safety of ezetimibe coadministered with lovastatin in primary hypercholesterolemia.	2003-02-15	12586255
Beyond statins. New drugs can work with, or in place of, cholesterol-lowering statins.	2003-02	12604459
Fresh from the pipeline. Ezetimibe.	2003-02	12572539
[Lowering cholesterol becomes easier. Combining instead of increasing dosage].	2003-01-23	12619241
[The best of clinical pharmacology in 2002].	2003-01	12613362
A novel therapeutic approach to dyslipidemia.	2003-01	12572626
Combination therapy for dyslipidemia.	2003-01	12572624
Treating hypercholesterolemia: looking forward.	2003-01	12539819
The intestinal absorption of biliary and dietary cholesterol as a drug target for lowering the plasma cholesterol level.	2003	12624559
Low-density lipoprotein lowering therapy: an analysis of the options.	2002-12-18	12505225
Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia.	2002-12-18	12505224
Management of dyslipidemia in the high-risk patient.	2002-12	12486415
[Cholesterol resorption inhibition prevents high statin doses. Lipid lowering in double-pack].	2002-11-28	12532550
[Ezetimib plus statin combination. A strong duo].	2002-11-28	12532547
[Ezetimib--the first selective cholesterol resorption inhibitors. Strengthening of statins].	2002-11-28	12532546
Combination therapy for dyslipidemia: safety and regulatory considerations.	2002-11-20	12467940
Use of combination therapy for dyslipidemia: a lipid clinic approach.	2002-11-20	12467939
[Improved antilipemic drug is approved. Cholesterol absorption is inhibited].	2002-11-14	12534088
Gateways to clinical trials.	2002-11	12616707
Gateways to clinical trials.	2002-10	12500432
Molecule of the month. Ezetimibe.	2001-04	12819822

Patents

Sample Use Guides

In Vivo Use Guide

10 mg orally once a day

Route of Administration: Oral

In Vitro Use Guide

10uM/L ezetimibe treatment of Huh7 hepatocytes significantly decreased PA-induced fat accumulation and increased PA-reduced mRNA and protein expression involved in autophagy

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:14:41 GMT 2025` Edited by `admin` on `Mon Mar 31 18:14:41 GMT 2025`
Record UNII	EOR26LQQ24
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

VYTORIN COMPONENT EZETIMIBE

Preferred Name

English

Ezetimibe

Official Name

English

Ezetimibe [USP MONOGRAPH]

Common Name

English

Ezetimibe [JAN]

Common Name

English

Ezetimibe [USAN]

Common Name

English

Ezetimibe [USP-RS]

Common Name

English

Ezetimibe [VANDF]

Common Name

English

SCH-58235

Code

English

SCH58235

Code

English

ROSZET COMPONENT EZETIMIBE

Brand Name

English

Ezetimibe [MI]

Common Name

English

NEXLIZET COMPONENT EZETIMIBE

Brand Name

English

NSC-758923

Code

English

(3R,4S)-1-(4-Fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-2-azetidinone

Systematic Name

English

Ezetimibe [ORANGE BOOK]

Common Name

English

Ezetimibe [MART.]

Common Name

English

ZETIA

Brand Name

English

Ezetrol

Brand Name

English

MK0653

Code

English

Ezetimibe [HSDB]

Common Name

English

Ezetimibe [WHO-DD]

Common Name

English

2-Azetidinone, 1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-, (3R,4S)-

Systematic Name

English

K-924 component Ezetimibe

Common Name

English

Ezetimibe [INN]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000008553