Lowering ‘LDL-C’ gets a boost with breakthrough drug

A new drug that will reinforce physicians’ existing therapeutic tools in lowering a patient’s low-density lipoprotein (LDL-C) or the bad cholesterol, is now out in the market.

Ezetimibe, launched by Schering-Plough Phils. Inc., has been shown to have a clinically significant supplementary effect when used with a statin, reducing LDL-C by an additional 25 percent.

Dr. Werner Katzmann, Far East regional medical director of the Schering-Plough Research Institute, presented scientific clinical data on the effectiveness and safety of ezetimibe in a lecture during the joint annual convention of the Philippine Society of Hypertension and Philippine Lipid Society recently.

Statins are currently prescribed as the most potent drug to lower LDL-C and prevent heart attacks and strokes, particularly in high-risk patients.

Attainment of recommended optimal levels of LDL-C, however, could not be achieved in a big number of patients with cholesterol problems.

According to Katzmann, a combination therapy of 10 mg ezetimibe with a very low dose of simvastatin has been shown to result in a 52 percent LDL-C reduction. The combination resulted in an 18 to 20 percent further reduction compared to monotherapy with simvastatin.

This will help patients achieve their guideline targets for cholesterol reduction without having to increase their statin dosage, Katzmann said.

Ezetimibe is the first in a new class of cholesterol-lowering drugs known as cholesterol absorption inhibitors (CAI) that block the transport of both dietary and biliary cholesterol across the intestinal wall. It prevents cholesterol from being re-absorbed by the body from the bowel. This leads to a reduction in the cholesterol delivered to the liver.

What statin can do only is work on the liver but it does not work on the small intestines where cholesterol absorption happens.

"Ezetimibe works on one pathway, while statins work on another pathway, and the combination provides the desired results via dual inhibition," Katzmann said.

Cholesterol management by administering statin is important in treating cardiovascular diseases (CVDs) and its complications such as heart attack and stroke. However, some patients experience side-effect or tolerance problems with higher doses of statins.

Ezetimibe optimizes the LDL-lowering effects of statins with a favorable tolerability profile. It can be taken any time of the day with or without food, and may be taken at the same time with any statin.

Currently approved in eight countries, including the United States, once-daily ezetimibe 10 mg is indicated in co-administration with a statin as adjunctive therapy to diet in patients with primary hypercholesterolemia.