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Monotherapy 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 (monotherapy), Primary hyperlipidemia.
At a glance
| Generic name | Monotherapy ezetimibe |
|---|---|
| Sponsor | NewAmsterdam Pharma |
| 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 (monotherapy)
- Primary hyperlipidemia
Common side effects
- Headache
- Fatigue
- Diarrhea
- Abdominal pain
Key clinical trials
- Moderate-intensity Statin vs. Individualized LDL-C Target-based Therapy in Older Adults With Type 2 Diabetes (iTARGET-Elderly Study) (NA)
- A Study to Evaluate the Effect of Obicetrapib/Ezetimibe 10 mg Fixed-Dose Combination or Obicetrapib 10 mg Daily on Top of Guideline-Recommended Lipid-Lowering Therapy in Participants With Type 2 Diabetes and/or Metabolic Syndrome (PHASE3)
- Efficacy and Safety of Pitavastatin/Ezetimibe After Switching From Statin Monotherapy to Pitavastatin/Ezetimibe in Patients With Hypercholesterolemia
- Long-term Comparison of Pitavastatin/Ezetimibe and Pitavastatin in Patients With Hypercholesterolemia and Elevated Triglycerides (PHASE4)
- Optimal Antiplatelet and Lipid Therapy in ACS With DES: OPACT Trial (NA)
- Effect of High-intensity Statin With Ezetimibe COmbination theRapy Versus High-intensity sTatin Monotherapy After Percutaneous Coronary Intervention With Drug-eluting Stents; the ESCORT Trial (NA)
- Early Statin-Ezetimibe Combination vs. Statin Monotherapy in Stroke With Atherosclerosis (PHASE2)
- Effects of Ezetimibe Combination Therapy for Patients With Atherosclerotic Cardiovascular Disease; Randomized Comparison of LDL-cholesterol Targeting <70 Versus <55mg/dL; Ez-PAVE Trial (NA)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Monotherapy ezetimibe CI brief — competitive landscape report
- Monotherapy ezetimibe updates RSS · CI watch RSS
- NewAmsterdam Pharma portfolio CI