No lipid increase with Merck integrase inhibitor at 24 weeks

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Participants receiving the new Merck integrase inhibitor MK-0518 experienced no significant increases in total cholesterol and triglycerides in a phase IIB dose-ranging study in treatment-naïve patients, presented on Wednesday at the Forty-Sixth Interscience Conference on Antimicrobial Agents and Chemotherapy in San Francisco.

The study compared four doses of MK-0518 with efavirenz in 184 treatment-naïve individuals also receiving tenofovir and 3TC. Preliminary twenty-four week efficacy results were presented last month at the Sixteenth International AIDS Conference in Toronto.

MK-0518 inhibits the activity of integrase, an HIV enzyme that allows the virus to insert its genetic material into the DNA of human T-cells. Preliminary results have shown that the drug is highly effective in suppressing HIV replication in both treatment-naïve and highly treatment-experienced patients.

Glossary

cholesterol

A waxy substance, mostly made by the body and used to produce steroid hormones. High levels can be associated with atherosclerosis. There are two main types of cholesterol: low-density lipoprotein (LDL) or ‘bad’ cholesterol (which may put people at risk for heart disease and other serious conditions), and high-density lipoprotein (HDL) or ‘good’ cholesterol (which helps get rid of LDL).

naive

In HIV, an individual who is ‘treatment naive’ has never taken anti-HIV treatment before.

lipid

Fat or fat-like substances found in the blood and body tissues. Lipids serve as building blocks for cells and as a source of energy for the body. Cholesterol and triglycerides are types of lipids.

treatment-naive

A person who has never taken treatment for a condition.

triglycerides

A blood fat (lipid). High levels are associated with atherosclerosis and are a risk factor for heart disease.

 

Baseline lipid levels were comparable across the five study arms, at around 160mg/mL for total cholesterol and between 110 and 155mg/dL for triglycerides.

After 24 weeks on treatment very slight declines in lipid levels were observed in the MK-0518 recipients at all doses (with the exception of HDL cholesterol), but in the efavirenz group all lipid levels rose. The only statistically significant difference was seen in LDL cholesterol, where the efavirenz group had an increase of approximately 5mg/dL whilst slight declines were seen at all MK-0518 doses (p

References

Teppler H et al. Differential effects of MK-0518 and efavirenz on serum lipids and lipoproteins in antiretroviral therapy-naïve patients. 46th ICAAC, San Francisco, abstract H-265a, 2006.