Ezetimibe
This oral medication reduces cholesterol levels by blocking its absorption from food in the small intestine, lowering the amount of cholesterol that reaches the liver and bloodstream. It is often used alongside a statin for greater cholesterol reduction.
Molecular Weight
409.4000 g/mol
LogP
4.00
TPSA
60.80 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
2D Structure
Cite this structure
Embed this structure
SMILES
O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1
InChI
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
Molecular Formula
C24H21F2NO3
HBD / HBA
2 / 5
Rotatable Bonds
6
Heavy Atoms
30
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
This oral medication reduces cholesterol levels by blocking its absorption from food in the small intestine, lowering the amount of cholesterol that reaches the liver and bloodstream. It is often used alongside a statin for greater cholesterol reduction.
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
Yes, Ezetimibe is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1138. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 150311. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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