OBJECTIVES: To estimate cost-effectiveness of rosuvastatin (RSV) versus atorvastatin (ATV); simvastatin (SMV), and pravastatin (PRV) in managing lipid profile parameters from a Canadian system perspective. METHODS: Annual cost-effectiveness ratios of RSV, ATV, SMV, and PRV were estimated in patients with hypercholesterolemia in terms of cost per percent LDL-C and TC/HDL-C and ApoB/ApoA-I reductions and Canadian guideline LDL-C goal attainment. Efficacy data were from a randomized, open-label trial including 2,268 adults (Jones et al, 2004). Drug costs [Can$, branded ATV and RSV; generic (g) SMV and gPRV] and dose utilization pattern within each statin from the Canadian province of British Columbia (March 2007) were used. Probabilistic sensitivity analysis was performed. RESULTS: RSV10 had lowest annual cost per percent reduction in LDL-C ($10.79), TC/HDL ($13.29) and ApoB/ApoA-I ($12.11), followed by gSMV80 ($11.19, $14.00, $13.20). After aggregating statin doses based on utilization pattern, RSV provided lowest mean annual cost per percent reduction in LDL-C ($11.03), TC/HDL ($13.55) and ApoB/ApoA-I ($12.39), followed by gSMV ($14.04, $16.96, $15.90), ATV ($16.93, $20.81, $19.48) and gPRV ($16.98, $20.01, $17.84), respectively. Cost per patient at goal was lowest for RSV ($603.46) followed by gPRV ($687.23), gSMV ($719.67) and ATV ($934.12). RSV was more effective and less costly than ATV on all assessed effectiveness measures. Comparing rosuvastatin to gSMV and gPRV, the value of an additional one percent reduction in LDL-C was $2.11 and $3.99, TC/HDL was $2.72 and $5.17, ApoB/ApoA-I was $2.30 and $4.88, and per one additional patient to goal was $143.64 and $373.91, respectively. Cost-effectiveness acceptability curve showed that RSV was the most cost-effective statin over a broad range of “willingness-to-pay” values per unit of clinical effect. CONCLUSION: Irrespective of effectiveness measure chosen, rosuvastatin can be considered as most cost-effective statin compared with atorvastatin, generic simvastatin and generic pravastatin in the Canadian province of British Columbia.