Add-on therapy for hypercholesterolemia: a pilot comparison of two gastrointestinally-acting agents in statin-treated patients.

BACKGROUND

Both colesevelam hydrochloride (colesevelam) and ezetimibe monotherapy have been reported to lower low-density lipoprotein cholesterol (LDL-C) approximately 15-17% in patients with hypercholesterolemia. When statin therapy is inadequate to reach desired LDL-C goals, the choice of add-on therapy, while multifactorial, must consider efficacy of additional LDL-C reduction.

OBJECTIVE

To provide pilot study data in assessing the relative potential of ezetimibe or colesevelam to further reduce LDL-C in statin-treated patients.

METHODS

Fourteen patients with hypercholesterolemia, who at baseline were on treatment with a stable regimen of low- to moderate-dose statin therapy, were randomized to receive colesevelam HCl 3.75 g/day or ezetimibe 10 mg/day as add-on therapy (AOT). At the end of 6 weeks, each patient was crossed over to the alternative AOT.

RESULTS

LDL cholesterol fell an additional 21.0% on colesevelam (P < .001) and 28.3% on ezetimibe (P <.001) with a 7.3% difference between AOTs (P <.02). Non-high-density lipoprotein cholesterol (non-HDL-C) fell an additional 15.1% on colesevelam (P <.001) and 25.6% on ezetimibe (P <.001) with a 10.5% difference between AOTs (P <.001). The non-HDL-C/HDL-C ratio fell an additional 15.3% on colesevelam (P <.01) and 22.8% on ezetimibe (P <.001) with a 7.5% difference between AOTs (P <.02). Zero of 10 and six of 10 secondary prevention patients reached an LDL-C level of <70 mg/dl on colesevelam and ezetimibe respectively (P <.005).

CONCLUSION

Colesevelam HCl and ezetimibe are both effective AOTs in patients on statin therapy. The superior further improvement in the lipid panel with ezetimibe compared to colesevelam was demonstrated in this placebo uncorrected crossover pilot study.