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MK0653, ezetimibe
Ezetimibe inhibits cholesterol absorption in the small intestine by blocking the Niemann-Pick C1-Like 1 (NPC1L1) transporter.
Ezetimibe inhibits cholesterol absorption in the small intestine by blocking the Niemann-Pick C1-Like 1 (NPC1L1) transporter. Used for Hypercholesterolemia (primary and secondary), Homozygous familial hypercholesterolemia, Heterozygous familial hypercholesterolemia.
At a glance
| Generic name | MK0653, ezetimibe |
|---|---|
| Sponsor | Organon and Co |
| Drug class | Cholesterol absorption inhibitor |
| Target | NPC1L1 (Niemann-Pick C1-Like 1) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Ezetimibe selectively binds to NPC1L1, a sterol transporter located on the brush border of the small intestine, preventing the uptake of dietary and biliary cholesterol. This reduces intestinal cholesterol absorption and leads to decreased plasma LDL cholesterol levels. The mechanism is distinct from statins, making ezetimibe useful as monotherapy or in combination with other lipid-lowering agents.
Approved indications
- Hypercholesterolemia (primary and secondary)
- Homozygous familial hypercholesterolemia
- Heterozygous familial hypercholesterolemia
Common side effects
- Headache
- Abdominal pain
- Diarrhea
- Fatigue
Key clinical trials
- Two Investigational Drugs in Patients With Mixed Hyperlipidemia (0653-036) (PHASE3)
- Open Label Study Evaluating The Use Of Combination Therapy Of Ezetimibe And Statins In Patients With Dyslipidemia In Colombia (0653-141)(COMPLETED) (PHASE4)
- MD Ezetimibe Cyclosporine Interaction (0653-057) (PHASE1)
- Study of an Approved Drug With a Statin (a Medication That Lowers Cholesterol Levels) as Compared to Statin Therapy Alone in Patients With High Cholesterol (0653-040) (PHASE3)
- Randomized Parallel Group Trial Of The Efficacy And Safety Of Ezetimibe With A Statin Versus Statin Dose Doubling In Patients With Persistent Primary Hypercholesterolemia (0653-152)(COMPLETED) (PHASE4)
- Study To Assess The Efficacy Of A Cholesterol Lowering Drug On Top Of Statins In Patients After Myocardial Infarction (MI)(0653A-150) (PHASE4)
- Study Evaluating the Efficacy and Safety of Simvastatin Alone Compared With Simvastatin Plus Ezetimibe in Type 2 Diabetic Patients (0653-021)(COMPLETED) (PHASE3)
- A Study Comparing Ezetimibe Plus Simvastatin Versus Simvastatin Alone in Patients at Risk for Heart Disease (0653-023)(COMPLETED) (PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |