Ezetimibe is marketed by Schering-Plough and Merck under the trade names Ezetrol and Zetia; there is also a combination pill, Vytorin, that contains ezetimibe plus simvastatin.

Ezetimibe lowers blood cholesterol levels by blocking cholesterol absorption in the intestine. Its effectiveness for this purpose have been demonstrated in HIV negative people, but data on ezetimibe in HIV positive individuals are limited.

As reported in the May 15, 2008, advance online edition of AIDS Patient Care and STDs, researchers at Temple University School of Medicine in Philadelphia enrolled HIV positive adults in a prospective, non-controlled pilot study to determine if their low-density lipoprotein (LDL) cholesterol was above the goal level despite statin therapy.

The study enrolled 20 participants; 12 (60%) were men and 18 (90%) were African American. All participants were required to be on stable protease inhibitor (PI)-based HAART and a low-dose statin. Seventeen patients (85%) were taking ritonavir-boosted PIs, while 3 (15%) were taking nelfinavir (Viracept).

The primary endpoint was LDL reduction at 18 weeks. In a subgroup of patients on lopinavir/ritonavir (Kaletra), trough concentrations were obtained before and after addition of ezetimibe.

Results

• Mean percentage changes from baseline in LDL were -10.9%, -12.2%, and -12.4% at weeks 6, 12, and 18, respectively (P < 0.05 for each time period vs. baseline).

• Mean percentage changes from baseline in total cholesterol were -11.1%, ?9.6%, and 9.1% at weeks 6, 12, and 18, respectively (P < 0.05 at each time period vs. baseline).

• No significant changes in triglycerides or high-density lipoprotein (HLD) were observed.

• Changes in lopinavir/ritonavir concentrations were not seen.

• 1 patient experienced elevated creatine phosphokinase (CPK) possibly related to study medication.

• No other adverse effects were seen.

Conclusion

In conclusion, the study authors wrote, "Addition of ezetimibe to low-dose statin effectively lowers LDL and total cholesterol and appears to be safe and well tolerated."

"In summary," they added, "Initiation of ezetimibe in HIV-infected patients on a PI and statin therapy effectively decreases LDL and total cholesterol. Because of our study limitations, these results should be further validated in larger clinical trials, but the use of ezetimibe should be considered" for HIV-infected HAART-treated patients with elevated lipids that do not respond to statins alone.

Department of Medicine, Temple University School of Medicine, Philadelphia, PA.

6/03/08

Reference
M Van Den Berg-Wolf, OM Klibanov, JP Gaughan, and others. Ezetimibe Combined with Low-Dose Statin Effectively Lowers LDL in Protease Inhibitor Treated Patients. AIDS Patient Care and STDs. May 15, 2008 [Epub ahead of print].