Rosuvastatin for the treatment of patients with hypercholesterolemia.

Objective: To review the currently available information on rosuvastatin in the treatment of primary hypercholesterolemia.

Data Sources: MEDLEY (2000-January 2001), MEDLIT, MEDLINE, EMBASE, SciSearch, Current Contents, Derwent, Drug, BIOSIS, Adis LMS Drug Alerts, and International Pharmaceutical Abstracts (1994-July 2001) were searched; unpublished data obtained from the manufacturer were also included.

Study Selection: Studies evaluating rosuvastatin including abstracts, proceedings, and data on file from the manufacturer were considered for inclusion. English-language literature was evaluated for pharmacology, pharmacodynamics, pharmacokinetics, therapeutic use, and adverse effects of rosuvastatin. Additional relevant citations were used in the introductory material and discussion section.

Data Extraction: English-language study abstracts selected for inclusion were limited to those on human subjects. Animal data were included only if human data were not available.

Data Synthesis: Resuvastatin, a new synthetic hydroxymethylglutaryl coenzyme A reductase inhibitor (HMG-CoA RI), recently completed Phase III clinical trials. At a dosage of 1-80 mg/d, the drug significantly reduced total cholesterol and low-density-lipoprotein cholesterol (LDL-C) and produced beneficial effects on other lipid parameters as well. Overall, resuvastatin was well tolerated.

Conclusions: In hypercholesterolemic patients, rosuvastatin reduced LDL-C and other lipid parameters to a greater degree than currently available agents. One advantage of rosuvastatin is that it achieves target LDL-C goals in a greater proportion of treated patients with similar adverse events compared with those treated with other HMG-CoA RIs. The potential to reduce risk of coronary heart disease events and decrease mortality as well as cost comparisons with currently used HMG-CoA RIs remains a subject of further investigation.