General Information

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.)

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.