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Rosuvastatin (Crestor)
Rosuvastatin inhibits HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step of cholesterol synthesis in the liver.
Rosuvastatin inhibits HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step of cholesterol synthesis in the liver. Used for Hypercholesterolemia and mixed dyslipidemia, Primary prevention of cardiovascular disease in at-risk patients, Secondary prevention of cardiovascular events in patients with established coronary heart disease.
At a glance
| Generic name | Rosuvastatin (Crestor) |
|---|---|
| Also known as | Crestor |
| Sponsor | Minneapolis Heart Institute Foundation |
| Drug class | HMG-CoA reductase inhibitor (statin) |
| Target | HMG-CoA reductase |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
By blocking HMG-CoA reductase, rosuvastatin reduces intracellular cholesterol levels, which triggers upregulation of LDL receptors on hepatocytes. This increases the clearance of LDL cholesterol from the bloodstream, resulting in significant reductions in plasma LDL-C, total cholesterol, and triglycerides. Rosuvastatin is a high-potency statin with superior LDL-lowering efficacy compared to many other statins.
Approved indications
- Hypercholesterolemia and mixed dyslipidemia
- Primary prevention of cardiovascular disease in at-risk patients
- Secondary prevention of cardiovascular events in patients with established coronary heart disease
Common side effects
- Myalgia (muscle pain)
- Headache
- Asthenia (weakness)
- Elevated liver enzymes (ALT/AST)
- Rhabdomyolysis (rare)
Key clinical trials
- Study to Evaluate the Effect of Repotrectinib on the Drug Levels of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants (PHASE1)
- Modular Clinical Pharmacology Study to Evaluate the Drug-drug Interaction Potential and Relative Bioavailability of Saruparib (PHASE1)
- A Clinical Study of the Effect of MK-2828 on Rosuvastatin or Furosemide in Healthy People (MK-2828-005) (PHASE1)
- Polygenic Risk-based Detection of Subclinical Coronary Atherosclerosis and Intervention With Statin and Colchicine (PHASE4)
- A Clinical Study of Enlicitide in Participants With High Cholesterol (MK-0616-037) (PHASE3)
- A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events (PHASE3)
- A Clinical Trial of Enlicitide and Rosuvastatin in Healthy Adults (MK-0616-039) (PHASE1)
- A Study to Investigate the Effect of AZD0780 Tablets in Combination With Rosuvastatin Tablets on Low Density Lipoprotein Cholesterol Levels (LDL-C) in Adult Participants With Dyslipidaemia (PHASE2)
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 (Crestor) CI brief — competitive landscape report
- Rosuvastatin (Crestor) updates RSS · CI watch RSS
- Minneapolis Heart Institute Foundation portfolio CI