5.8. Treatment of hyhpercholesterolemia

5.8.1. RS-86505-007

The lower dose of RS-86505-007, 3 mg three times daily, showed a trend towards lower total and LDL cholesterol. RS-86505-007 at a dose of 6 mg three times daily produced a highly significant decreases in total and LDL cholesterol in patients with good compliance at all time points, resulting in mean reductions of 14.6 % (5% confidence interval 1.4-23.8, p=0.03) for total cholesterol and 18.5 % (95% confidence interval 2.1-28.8, p=0.03) for LDL cholesterol at six weeks. There were no consistent trends for HDL chole­sterol or triglycerides.

Compliance with and side-effects of RS-86505-007 are shown in Table 5-9. At both dose levels, around two thirds of the side-effects were related to the gastrointestinal system. The higher dose of the drug compared to the lower dose doubled the percentage of patients reporting side-effects (81% in the drug-treated vs. 46% in the placebo group). In addition, the frequency of side-effects per patient was higher in the drug-treated group (53 side-effects in 21 patients) than in the placebo group (9 side-effects in 6 patients). Four patients dropped out prematurely due to side-effects, one in the 3 mg and three in the 6 mg group due to gastrointestinal disturbances, and one patient also had moderate menorrhagia.

Table 5-9. Compliance and adverse events.

 RS-86505-0073 mg tidRS-86505-0076 mg tid
active drug N=24placebo N=12active drug N=26placebo N=13
Poor compli­ance*25 %33 %31 %0 %
Events3217539
Mild149164
Moderate138305
Severe2030
Dropouts due to side-effects1030
* Consumption of less than 78% of capsules delivered The severity of adverse events was not recorded in 3 patients in the 3 mg group and 4 patients in the 6 mg group

5.8.2. Lovastatin and colestipol

Lovastatin lowered both total and LDL cholesterol more effectively than colestipol, but the drugs were equally effective in elevating HDL cholesterol, whereas triglycerides were slightly elevated during the colestipol treatment and lowered during the lovastatin treatment (Table 5-10). The patients also lost some weight during the colestipol treatment, but started gain

Table 5-10. Lipid values of patients at baseline and after colestipol and lovastatin treatment.

 BaselineColestipolLovastatinp*
Total cholesterol, mmol/l8.89(1.62)6.54(1.36)5.87(1.11)0.0001
LDL cholesterol, mmol/l6.78(1.73)4.32(1.46)3.81(1.18)0.0001
HDL cholesterol, mmol/l1.39(0.37)1.46(0.45)1.48(0.37)0.44
Triglycerides, mmol/l1.59(0.58)1.78(0.80)1.31(0.58)0.0001
The values are expressed as mean (SD). * significance for the difference between colestipol and lovastatin treatment.