MedPath

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

Overview

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.

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

Clinical Trials

View More Clinical Trials

Sign in to access the complete clinical trial database with detailed study information.

Title
Posted
Study ID
Phase
Status
Sponsor
2013/03/08
Phase 4
UNKNOWN
University of Roma La Sapienza
2013/01/11
Phase 2
Completed
2013/01/09
Phase 3
Completed
2013/01/09
Phase 3
Completed
2013/01/09
Phase 3
Completed
2012/11/21
Phase 3
Completed
2012/11/21
Phase 3
Completed
2012/11/08
Phase 1
Completed
2012/10/18
Phase 3
Completed
2012/07/19
Phase 3
Completed

FDA Drug Approvals

View More FDA Approvals

Sign in to access additional FDA-approved drug information with detailed regulatory data.

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
NORTHSTAR RX LLC
16714-781
ORAL
10 mg in 1 1
11/30/2020
A-S Medication Solutions
50090-4772
ORAL
10 mg in 1 1
11/30/2021
Esperion Therapeutics, Inc.
72426-818
ORAL
10 mg in 1 1
3/28/2024
Amneal Pharmaceuticals NY LLC
60219-1157
ORAL
10 mg in 1 1
1/28/2022
Organon LLC
78206-176
ORAL
10 mg in 1 1
2/8/2024
Proficient Rx LP
82804-211
ORAL
10 mg in 1 1
3/1/2025
Preferred Pharmaceuticals Inc.
68788-8297
ORAL
10 mg in 1 1
5/25/2023

EMA Drug Approvals

View More EMA Approvals

Sign in to access additional EMA-approved drug information with detailed regulatory data.

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

View More HSA Approvals

Sign in to access additional HSA-approved drug information with detailed regulatory data.

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

View More NMPA Approvals

Sign in to access additional NMPA-approved drug information with detailed regulatory data.

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

View More PPB Approvals

Sign in to access additional PPB-approved drug information with detailed regulatory data.

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

View More TGA Approvals

Sign in to access additional TGA-approved drug information with detailed regulatory data.

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
EZETIMIBE - ROSUVASTATIN SANDOZ 10 MG / 40 MG ezetimibe 10 mg tablets and rosuvastatin (as calcium) 40 mg tablets composite pack
318873
Medicine
A
7/7/2022
EZALO Composite Pack 10mg+10mg ezetimibe 10mg tablets and rosuvastatin (as calcium) 10mg tablets composite pack
203689
Medicine
A
11/26/2013
EZETIMIBE/SIMVASTATIN SANDOZ 10/40 ezetimibe/simvastatin 10/40 mg tablet blister pack
279098
Medicine
A
11/6/2017
EZETIMIBE/SIMVASTATIN SANDOZ 10/80 ezetimibe/simvastatin 10/80 mg tablet blister pack
279117
Medicine
A
11/6/2017
EZETIMIBE GH ezetimibe 10 mg tablet bottle (HDPE bottle with molecular sieve sachet)
246024
Medicine
A
7/4/2016
EZETIMIBE/ATORVASTATIN GENERICHEALTH 10/20 ezetimibe and atorvastatin (as calcium trihydrate) 10 mg/20 mg tablets blister pack
306960
Medicine
A
11/1/2019
SIMTORSI 10/20 ezetimibe 10 mg and simvastatin 20 mg tablet blister pack
309735
Medicine
A
10/15/2019
EZETIMIBE/ATORVASTATIN GH 10/20 ezetimibe and atorvastatin (as calcium trihydrate) 10 mg/20 mg tablets blister pack
306957
Medicine
A
11/1/2019
EZETIMIBE-SIMVASTATIN ALPHAPHARM 10/80 ezetimibe 10 mg and simvastatin 80 mg tablet blister pack
206634
Medicine
A
1/11/2021
EZECREST COMPOSITE PACK 10 mg+10 mg ezetimibe 10 mg tablet and rosuvastatin (as calcium) 10 mg tablet blister composite pack
375662
Medicine
A
2/6/2023
© Copyright 2025. All Rights Reserved by MedPath