Last reviewed · How we verify
Rosuvastatin active capsule
Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis, thereby reducing LDL cholesterol levels.
Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis, thereby reducing LDL cholesterol levels. Used for Hypercholesterolemia and dyslipidemia, Primary prevention of cardiovascular disease, Secondary prevention of cardiovascular events in patients with established coronary artery disease.
At a glance
| Generic name | Rosuvastatin active capsule |
|---|---|
| Sponsor | Sanofi |
| Drug class | HMG-CoA reductase inhibitor (statin) |
| Target | HMG-CoA reductase |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Rosuvastatin is a statin that competitively inhibits HMG-CoA reductase, blocking the conversion of HMG-CoA to mevalonate in the cholesterol biosynthetic pathway. This leads to decreased intracellular cholesterol production, upregulation of LDL receptors on hepatocytes, and increased clearance of LDL cholesterol from the bloodstream. The net result is significant reduction in serum LDL cholesterol and triglycerides, with modest increases in HDL cholesterol.
Approved indications
- Hypercholesterolemia and dyslipidemia
- Primary prevention of cardiovascular disease
- Secondary prevention of cardiovascular events in patients with established coronary artery disease
Common side effects
- Myalgia (muscle pain)
- Elevated liver enzymes (ALT/AST)
- Headache
- Rhabdomyolysis (rare)
- Nausea
Key clinical trials
- Polygenic Risk-based Detection of Subclinical Coronary Atherosclerosis and Intervention With Statin and Colchicine (PHASE4)
- A Study to Evaluate the Efficacy and the Safety of Single Pill Combination (SPC) Ezetimibe/Rosuvastatin in Chinese Adult Patients With Primary Hypercholesterolemia Not Adequately Controlled on Statin Therapy (PHASE3)
- Polypill and RiscOMeter to Prevent StrOke and CogniTive ImpairmEnt (PROMOTE) (PHASE3)
- A Study of the Efficacy and Safety of MK-0653H in Japanese Participants With Hypercholesterolemia (MK-0653H-832) (PHASE3)
- A 3-part Study to Evaluate Safety, Tolerability, Food Effect and Drug-drug Interactions of RXC007 in Healthy Volunteers (PHASE1)
- Use of Rosuvastatin in HIV-Infected Subjects to Modulate Cardiovascular Risks (PHASE2)
- Collaborative H1N1 Adjuvant Treatment (CHAT) Pilot Trial (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 |