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Ezetimibe

Generic Name
Ezetimibe
Brand Names
Ezetrol, Lypqozet, Nexlizet, Roszet, Vytorin, Zetia
Drug Type
Small Molecule
Chemical Formula
C24H21F2NO3
CAS Number
163222-33-1
Unique Ingredient Identifier
EOR26LQQ24
Background

Ezetimibe is a lipid-lowering compound that inhibits intestinal cholesterol and phytosterol absorption. The discovery and research of this drug began in the early 1990s, after the intravenous administration of radiolabelled ezetimibe in rats revealed that it was being localized within enterocytes of the intestinal villi - this prompted studies investigating the effect of ezetimibe on intestinal cholesterol absorption. Ezetimibe is used as an adjunctive therapy to a healthy diet to lower cholesterol levels in primary hyperlipidemia, mixed hyperlipidemia, homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia (phytosterolemia).

Unlike other classes of cholesterol-reducing compounds including statins and bile acid sequestrants, ezetimibe has a distinct mechanism of action involving the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), and is unique in that it does not affect the absorption of fat-soluble nutrients such as fat-soluble vitamins, triglycerides, or bile acids. In genetically NPC1L1-deficient mice, a 70% reduction in intestinal cholesterol absorption was seen, and these mice were insensitive to ezetimibe treatment - it was determined based on these findings that NPC1L1 plays an essential role in promoting intestinal cholesterol uptake via an ezetimibe-sensitive pathway. By interfering with the intestinal uptake of cholesterol and phytosterols, ezetimibe reduces the delivery of intestinal cholesterol to the liver.

Indication

Ezetimibe is indicated to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary hyperlipidemia, alone or in combination with an HMG-CoA reductase inhibitor (statin). It is also indicated to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in combination with fenofibrate, and to reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH), in combination with atorvastatin or simvastatin. Ezetimibe may also be used to reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia (phytosterolemia).

Associated Conditions
Elevated Blood Lipids, Elevated sitosterol and campesterol
Associated Therapies
-

Clinical Trial to Evaluate the Efficacy and Safety of CKD-391

Phase 3
Completed
Conditions
Hyperlipidemia
Interventions
Drug: Atorvastatin40mg, Ezetimibe placebo
Drug: Atorvastatin10mg, Ezetimibe10mg
Drug: Atorvastatin10mg, Ezetimibe placebo
Drug: Atorvastatin20mg, Ezetimibe10mg
Drug: Atorvastatin20mg, Ezetimibe placebo
Drug: Atorvastatin40mg, Ezetimibe10mg
First Posted Date
2015-05-21
Last Posted Date
2016-01-28
Lead Sponsor
Chong Kun Dang Pharmaceutical
Target Recruit Count
385
Registration Number
NCT02451098
Locations
🇰🇷

The catholic university of korea seoul st. Mary's hospital, Seoul, Korea, Republic of

Effects of Simvastatin and Ezetimibe on Cardiovascular Risk Markers in Patients With Dyslipidemia

Not Applicable
Completed
Conditions
Dyslipidemia
Interventions
First Posted Date
2014-12-02
Last Posted Date
2018-03-08
Lead Sponsor
Fundación para el Fomento de la Investigación Sanitaria y Biomédica de la Comunitat Valenciana
Target Recruit Count
42
Registration Number
NCT02304926

to Investigate the Pharmacokinetic Interactions and Safety Between Rosuvastatin and Ezetimibe in Healthy Male Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Ezetrol
Drug: Crestor+Ezetrol
Drug: Crestor
First Posted Date
2014-11-13
Last Posted Date
2016-03-25
Lead Sponsor
NVP Healthcare
Target Recruit Count
59
Registration Number
NCT02289430

A Study of Evacetrapib (LY2484595) in Combination With Atorvastatin in Japanese Participants With Primary Hypercholesterolemia

Phase 3
Terminated
Conditions
Hypercholesterolemia
Interventions
First Posted Date
2014-10-09
Last Posted Date
2018-10-09
Lead Sponsor
Eli Lilly and Company
Target Recruit Count
149
Registration Number
NCT02260648
Locations
🇯🇵

For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Tokyo, Japan

Effect of an Inhibitor of Cholesterol Absorption on Vitamin D Levels

Phase 4
Completed
Conditions
Vitamin D Deficiency
Interventions
First Posted Date
2014-09-09
Last Posted Date
2015-04-09
Lead Sponsor
Federal University of Rio Grande do Sul
Target Recruit Count
52
Registration Number
NCT02234544
Locations
🇧🇷

Hospital de Clínicas de Porto Alegre, Porto Alegre, RS, Brazil

A Study of Evacetrapib (LY2484595) in Participants With High Cholesterol

Phase 3
Terminated
Conditions
Hyperlipidemia
Interventions
First Posted Date
2014-08-28
Last Posted Date
2019-10-08
Lead Sponsor
Eli Lilly and Company
Target Recruit Count
366
Registration Number
NCT02227784
Locations
🇺🇸

Alan Graff, MD, PA, Fort Lauderdale, Florida, United States

🇺🇸

Northwest Heart Clinical Research, LLC, Arlington Heights, Illinois, United States

🇺🇸

Maryland Cardiovascular Specialists, Baltimore, Maryland, United States

and more 60 locations

Rosuvastatin for Reduction of Myocardial Damage and Systemic Inflammation During Coronary Angioplasty

Phase 3
Terminated
Conditions
Stable Coronary Artery Disease Undergoing PCI
Interventions
First Posted Date
2014-07-31
Last Posted Date
2014-07-31
Lead Sponsor
G. d'Annunzio University
Target Recruit Count
280
Registration Number
NCT02205775
Locations
🇮🇹

Azienda ASL 6 - P. Ospedaliero Livorno, Livorno, Italy

🇮🇹

Azienda Ospedaliera - Ospedale San Paolo, Milano, Italy

🇮🇹

Fondazione IRCCS Policlinico S. Matteo, Pavia, PV, Italy

and more 3 locations

Pilot Study of Ezetimibe for Chronic Hepatitis C Virus (HCV) Infection

Phase 1
Conditions
Chronic Hepatitis C
Interventions
First Posted Date
2014-04-29
Last Posted Date
2015-11-04
Lead Sponsor
Pontificia Universidad Catolica de Chile
Target Recruit Count
20
Registration Number
NCT02126137
Locations
🇨🇱

Department of Gastroenterology, Pontificia Universidad Católica de Chile, Santiago, Metropolitan, Chile

The Impact of Ezetimibe on Biochemical Markers of Cardiovascular Risk in Kidney Transplant Patients

Phase 4
Completed
Conditions
Dyslipidemia
Transplants
Interventions
First Posted Date
2014-04-03
Last Posted Date
2016-05-17
Lead Sponsor
University Medical Centre Ljubljana
Target Recruit Count
80
Registration Number
NCT02103049
Locations
🇸🇮

University Medical Center Ljubljana, Ljubljana, Slovenia

Plant Sterols Effect on Previous Statin Therapy

Phase 2
Completed
Conditions
Coronary Artery Disease
Interventions
Other: Ezetimibe + plant sterols
Dietary Supplement: Plant sterols
Drug: Ezetimibe
First Posted Date
2014-03-18
Last Posted Date
2014-03-19
Lead Sponsor
Jose Rocha Faria Neto
Target Recruit Count
47
Registration Number
NCT02089867
Locations
🇧🇷

Jose Rocha Faria Neto, Curitiba, Paraná, Brazil

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