Last reviewed · How we verify
Rosuvastatin and Ezetimibe
Rosuvastatin inhibits HMG-CoA reductase to lower LDL cholesterol, while ezetimibe blocks intestinal cholesterol absorption, providing dual lipid-lowering action.
Rosuvastatin inhibits HMG-CoA reductase to lower LDL cholesterol, while ezetimibe blocks intestinal cholesterol absorption, providing dual lipid-lowering action. Used for Hypercholesterolemia and dyslipidemia, Cardiovascular risk reduction in patients requiring additional LDL-C lowering.
At a glance
| Generic name | Rosuvastatin and Ezetimibe |
|---|---|
| Also known as | Crestor and Ezetrol |
| Sponsor | Hanmi Pharmaceutical Company Limited |
| Drug class | Statin and ezetimibe combination |
| Target | HMG-CoA reductase and NPC1L1 transporter |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Rosuvastatin is a statin that reduces cholesterol synthesis in the liver by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol production. Ezetimibe selectively inhibits cholesterol absorption in the small intestine by blocking the Niemann-Pick C1-like 1 (NPC1L1) transporter. Together, they provide complementary mechanisms to reduce both endogenous cholesterol production and dietary cholesterol uptake, resulting in greater LDL-C lowering than either agent alone.
Approved indications
- Hypercholesterolemia and dyslipidemia
- Cardiovascular risk reduction in patients requiring additional LDL-C lowering
Common side effects
- Myalgia
- Elevated liver enzymes
- Headache
- Gastrointestinal disturbance
Key clinical trials
- A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events (PHASE3)
- Moderate-intensity Statin vs. Individualized LDL-C Target-based Therapy in Older Adults With Type 2 Diabetes (iTARGET-Elderly Study) (NA)
- A Study of Bempedoic Acid in Combination With Ezetimibe and Either Rosuvastatin or Atorvastatin in Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia
- Optimal Antiplatelet and Lipid Therapy in ACS With DES: OPACT Trial (NA)
- Early Statin-Ezetimibe Combination vs. Statin Monotherapy in Stroke With Atherosclerosis (PHASE2)
- LATAM LOWERS LDL-C (PHASE4)
- Evaluating Bioequivalence of a Fixed Dose Combination Versus Tablets of Bempedoic Acid / Ezetimibe and Rosuvastatin (PHASE1)
- Effect of Intensive Lipid-Lowering Therapy on Coronary Atherosclerotic Plaque Progression in Young and Middle-Aged Patients With Chronic Coronary Syndrome (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:
- Rosuvastatin and Ezetimibe CI brief — competitive landscape report
- Rosuvastatin and Ezetimibe updates RSS · CI watch RSS
- Hanmi Pharmaceutical Company Limited portfolio CI