The combination of rosuvastatin and ezetimibe reduces low-density lipoprotein cholesterol beyond levels seen with previous trials while also reducing C-reactive protein levels, according to an article in the March issue of American Journal of Cardiology.

“A seventy percent drop is the largest reduction in bad cholesterol ever seen in a statin clinical trial. Cardiologists have long recognized the challenge in helping high-risk patients reach their target cholesterol levels, to ultimately prevent heart attack and stroke,” said Christie Ballantyne, MD, cardiologist at the Methodist DeBakey Heart Center and principal investigator. “These results offer hope for these patients.”

The EXPLORER (Examination of Potential Lipid modifying effects Of Rosuvastatin in combination with Ezetimibe versus Rosuvastatin alone) study was a 12-week, randomized trial of 469 patients with low-density cholesterol between 160 and 250 mg/dL (4.1-<6.5 mmol/L) and coronary heart disease risk equivalent designed to evaluate whether adding ezetimibe to rosuvastatin would enable more patients with severely high cholesterol to achieve guideline lipid goals compared with rosuvastatin monotherapy.

Patients participated in a six-week dietary lead-in followed by six weeks of randomized treatment with rosuvastatin 40 mg alone or in combination with ezetimibe 10 mg.

The combination of statins (40 mg rosuvastatin, 10 mg ezetimibe) reduced low-density lipoprotein cholesterol by an unprecedented 70 percent from baseline.
Significantly more patients achieved their goal of low-density lipoprotein cholesterol <100 mg/dL (94 percent vs. 79 percent) at six weeks with combination therapy compared with rosuvastatin monotherapy. In addition, combination therapy reduced C-reactive protein levels by 46 percent compared with 29 percent for rosuvastatin monotherapy.

Participants in both study arms had a similar increase in high-density lipoprotein cholesterol (8.5 percent vs. 10.8 percent).

Physicians have long relied on blood cholesterol as a key indicator of cardiovascular risk, but recent research suggests that high-risk patients who achieve a low C-reactive protein level combined with a low low-density lipoprotein cholesterol level had the fewest cardiovascular events.

“The highly effective reductions in both LDL-c and CRP seen in the EXPLORER study provide a new opportunity for high-risk patients to achieve optimal reduction in both factors with combination therapy,” Ballantyne said.