Currently Enrolling Trials
Crestor (rosuvastatin calcium) is a synthetic lipid-lowering agent approved as a treatment for hypercholesterolemia. The drug is classified as a Statin, a type of agent that inhibits cholesterol production in the liver.
Crestor is indicated for the following:
- for the treatment of hypercholesterolemia
- as adjunctive therapy to diet to slow the progression of atherosclerosis in adult patients as part of a treatment strategy to lower Total-C and LDL-C to target levels.
- to treat patients with primary dysbetalipoproteinemia (Fredrickson type III hyperlipoproteinemia) as an adjunct to diet.
- for the treatment of heterozygous familial hypercholesterolemia in adolescent boys and postmenarchal girls, ages 10 to 17 years, with a recommended dosing range of 5 to 20 mg once daily
- for the primary prevention of cardiovascular disease
- for treatment of pediatric patients 7 to 17 years of age with homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C, total C, nonHDL-C and ApoB as an adjunct to diet, either alone or with other lipid-lowering treatments.
Crestor is supplied as tablets for oral administration. Crestor can be taken with or without food, at any time of day.
Dose range: 5-40 mg once daily. Use 40 mg dose only for patients not reaching LDL-C goal with 20 mg.
- Adult HoFH: Starting dose 20 mg/day
- Pediatric patients with HeFH: 5 to 10 mg/day for patients 8 to less than 10 years of age, and 5 to 20 mg/day for patients 10 to 17 years of age.
- Pediatric patients with HoFH: 20 mg/day for patients 7 to 17 years of age
Mechanism of Action
Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
Rosuvastatin reduces cholesterol by increasing the number of low-density lipoprotein (LDL) receptors on the cell-surface to enhance uptake and catabolism of LDL. It also inhibits hepatic synthesis of hepatic very-low-density lipoprotein (VLDL), which reduces the total number of VLDL and LDL particles. The treatment reduces triglycerides (TG) and produces increases in high-density lipoprotein cholesterol (HDL-C.)
Adverse events associated with the use of Crestor may include (but are not limited to) the following:
- Back Pain
- Flu syndrome
- Urinary tract infection
Clinical Trial Results
FDA approval of Crestor was based a double-blind, placebo-controlled, dose-ranging study and a open-label study of 2,240 subjects with type IIa and IIb hypercholesterolemia. Results demonstrated that Crestor reduced total-C, LDL-C, ApoB, nonHDL-C, and TG, and increases HDL-C, in patients with hypercholesterolemia and mixed dyslipidemia.