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Crestor (rosuvastatin)
Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme converting HMG-CoA to mevalonate, a cholesterol precursor.
Rosuvastatin is an HMG-CoA reductase inhibitor indicated for reducing cardiovascular events and LDL-C across multiple patient populations including primary hyperlipidemia, atherosclerosis, and familial hypercholesterolemia. It demonstrates approximately 20% bioavailability with a 19-hour half-life and is primarily hepatically cleared (72%) with minimal renal excretion. Significant drug interactions exist with CYP2C9 and transporter inhibitors (cyclosporine, teriflunomide, enasidenib) requiring dose reductions to mitigate myopathy and rhabdomyolysis risk. Rosuvastatin is contraindicated in acute liver failure, decompensated cirrhosis, and hypersensitivity reactions, with careful monitoring required in severe renal impairment and Asian populations showing 2-fold higher exposure.
At a glance
| Generic name | rosuvastatin |
|---|---|
| Sponsor | AstraZeneca |
| Drug class | HMG-CoA reductase inhibitor (statin) |
| Target | HMG-CoA reductase |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 2003 |
Mechanism of action
Rosuvastatin is an inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. By inhibiting this enzyme, rosuvastatin reduces cholesterol synthesis in the liver. Greater than 90% of active plasma HMG-CoA reductase inhibitory activity is accounted for by the parent compound, with the major metabolite N-desmethyl rosuvastatin having approximately one-sixth to one-half the HMG-CoA reductase inhibitory activity of the parent compound.
Approved indications
- Arteriosclerotic vascular disease
- Cerebrovascular accident
- Familial hypercholesterolemia - heterozygous
- Familial hypercholesterolemia - homozygous
- Familial type 3 hyperlipoproteinemia
- Hypercholesterolemia
- Hypertriglyceridemia
- Mixed hyperlipidemia
- Myocardial Infarction Prevention
- Prevention of Transient Ischemic Attacks
- Primary Prevention of Coronary Heart Disease
Common side effects
- Headache
- Cough
- Nasal congestion
- Diarrhoea
- Abdominal pain lower
- Nausea
- Ligament sprain
- Decreased appetite
- Oropharyngeal pain
- Dizziness
- Haematoma
- Phlebitis
Drug interactions
- Cyclosporine
- Teriflunomide
- Enasidenib
- Aluminum and Magnesium Hydroxide Combination Antacids
- Warfarin
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Crestor CI brief — competitive landscape report
- Crestor updates RSS · CI watch RSS
- AstraZeneca portfolio CI