Research Sheds Light on Action of Cholesterol Drug Zetia
Tuesday June 19, 2007
Research conducted in mice is shedding new light on the inner workings of the powerful cholesterol busting drug Zetia (ezetimibe). An article published in the Journal of Clinical Investigation shows that Zetia appears to exhert the majority of its action in the liver and intestine, blocking both the processing and absorption of certain types of fats. It was previously believed that Zetia acted only the intestine, where it interferred with the uptake of fats consumed in the diet.
In both the liver and the intestine, Zetia targets a protein called NPC1L1, which is responsible for shuttling cholesterol directly into cells. It is thought that by blocking this action, the drug prevents the absorption of cholesterol into the body's metabolism pathways.
As evidence for this, researchers cite their use of genetically engineered mice which were bred to have high levels of NPC1L1. These mice had very high concentrations of cholesterol in their bile (a sign that it had been absorbed and processed by the liver) but treating the mice with Zetia caused dramatic reductions in bile cholesterol levels. Since NPC1L1 is the primary agent that transfers the cholesterol from liver to bile, the reduction seems to indicate that the drug acts on this protein within the liver.
Controlling cholesterol is an important part of maintaining a heart healthy diet, and is especially important for patients with high blood pressure, since they are at increased risk for cardiovascular disease.
Related: The DASH Diet for High Blood Pressure
In both the liver and the intestine, Zetia targets a protein called NPC1L1, which is responsible for shuttling cholesterol directly into cells. It is thought that by blocking this action, the drug prevents the absorption of cholesterol into the body's metabolism pathways.
As evidence for this, researchers cite their use of genetically engineered mice which were bred to have high levels of NPC1L1. These mice had very high concentrations of cholesterol in their bile (a sign that it had been absorbed and processed by the liver) but treating the mice with Zetia caused dramatic reductions in bile cholesterol levels. Since NPC1L1 is the primary agent that transfers the cholesterol from liver to bile, the reduction seems to indicate that the drug acts on this protein within the liver.
Controlling cholesterol is an important part of maintaining a heart healthy diet, and is especially important for patients with high blood pressure, since they are at increased risk for cardiovascular disease.
Related: The DASH Diet for High Blood Pressure
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