Home » Drug Information » FDA Approved Drugs » 2003
Medical Areas: Cardiology/Vascular Diseases
View By:YearCompanyConditionsTherapeutic AreasDrug Names
Crestor (rosuvastatin calcium)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Approval Status: Approved August 2003
Treatment Area: Hypercholesterolemia
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 as an adjunct to diet to reduce elevated
cholesterol levels in the blood. It is indicated for primary
hypercholesterolemia (heterozygous familial and nonfamilial) and
mixed dyslipidemia (Fredrickson Type IIa and IIb).
It is also indicated as an adjunct to diet for the treatment of
patients with elevated serum TG levels (Fredrickson Type IV) and in
patients with homozygous familial hypercholesterolemia as an
adjunct to other lipid-lowering treatments.
The dose range for Crestor is 5 to 40 mg once daily. Therapy
should be individualized according to goal of therapy and
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.
Adverse events associated with the use of Crestor may include
(but are not limited to) the following:
- Back Pain
- Flu syndrome
- Urinary tract infection
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.)
Davidson MH.. Rosuvastatin: a highly
efficacious statin for the treatment of dyslipidaemia. Expert
Opin Investig Drugs. 2002 Mar;11(3):125-41. Review.
McTaggart F. Comparative pharmacology of
rosuvastatin. Atheroscler Suppl.. 2003 Mar; 4(1):
Nezasa K, Higaki K, Takeuchi M, Nakano M, Koike
M. Uptake of rosuvastatin by isolated rat hepatocytes:
comparison with pravastatin. Xenobiotica. 2003 Apr; 33(4):
Stein EA. The power of statins: aggressive
lipid lowering. Clin Cardiol. 2003 Apr; 26(4 Suppl 3):