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CETP Inhibitors
CETP inhibitors are drugs / medications that raise HDL good cholesterol levels. Currently major research is going on by pharmaceutical companies to develop these CETP inhibiting drugs with minimal side effects. CETP inhibitors are the new approach in the fight against heart disease caused by cholesterol problems, as it is now recognised that it is the LDL bad cholesterol that causes heart disease and that HDL can actually help to reduce and even reverse the bad effects.
CETP
"CETP" stands for cholesteryl ester transfer protein . This protein is considered bad because it assists in moving cholesterol from the HDL good form to the bad LDL form. Because of the research that shows that raising HDL good cholesterol levels can actually decrease LDL bad cholesterol levels, inhibiting these CETP is a way to increase the HDL cholesterol levels. The CETP inhibitors are being looked at as a drug to be taken alone or along with the already widely used statin cholesterol drugs.
CETP Inhibitors Drugs to raise HDL Cholesterol Levels
Pfizer is developing a drug called torcetrapib and early results from trials are quite promising. The FDA is currently considering whether the drug can be marketed and results of those studies should be released in 2006.
An anti CETP vaccine is being developed by the company called Avant Pharmaceuticals and several other drug companies are also developing CETP inhibitors.
Research has shown that fibrates or niacin can raise HDL good cholesterol levels and it has been proved that this slows the progression and speeds regression of atherosclerosis in addition to reducing risk of heart attacks and heart disease. So the development of the CETP inhibitors to raise HDL would appear to be an important step in the fight against these diseases.
Doubts About CETP Inhibitors
Some experts still have doubts about the hypothesis that raising HDL cholesterol levels is important. They consider that HDL levels are merely a marker for coronary heart disease or believe that triglyceride levels, which are usually elevated when HDL cholesterol levels are low, are responsible for higher disease rates. However looking at the role HDL plays in reverse cholesterol transport shines a light on these doubts.
Low density lipoproteins transport cholesterol to arteries causing plaque build up and also to the liver. Reverse cholesterol transport refers to the movement of cholesterol from the arteries back to the liver where it can be washed out and HDL is essential for this process. High density lipoproteins actually remove cholesterol that has built up in the arteries. This reverse transport is mediated by cholesterol ester transfer protein (CETP), and that is why this enzyme has become the focus of intense research and drug development. Study of CETP in humans and in animal models has shown that it has an effect on proatherogenic and antiatherogenic actions.
Other New Cholesterol Drugs
Continuing research is revealing new mechanisms that are involved in the development of heart disease and as a response many new cholesterol drugs are being developed including the CETP inhibitors. New approaches aimed at modifying cholesterol and lipid balance in the body are under investigation.
Some of these potential medications are listed below :
- Lipoprotein-Associated Phospholipase A2 inhibitors (Lp-PLA2)
- Peroxisome Proliferator Activated Receptor stimulators (PPAR)
- Cholesteryl Ester Transfer Protein inhibitors(CETP) (see details above)
Lp-PLA2 mass may be a useful marker of sub-clinical cardiovascular risk, research continues.
The PPAR drug studies are not as far advanced as the CETP studies, they are a class of drugs being studied to raise HDL levels, that work by stimulating a pro-HDL gene.
All the research may take some years to draw firm conclusions but raising HDL good cholesterol levels is clearly an area that has been brought into focus, it is a major goal of the drug companies and a significant breakthrough in the prevention and maybe even reverse of coronary heart diseas looks to be inevevitable.
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