Torcetrapib and Rimonabant-Acomplia: Promising Next-Generation "Good" Cholesterol Raising Drugs

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Based on compelling evidence that raising high-density lipoprotein cholesterol levels (HDL-C, also known as "good" cholesterol) helps halt atherosclerosis, pharmaceutical companies are racing to produce the next generation of medications to replace the ineffectual ones currently on the market. Niacin, the current drug of choice, increases HDL-C by only 15% to 35%, and then only at daily doses three grams or higher, increasing the chance for unpleasant side effects.

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Based on compelling evidence that raising high-density lipoprotein cholesterol levels (HDL-C, also known as "good" cholesterol) helps halt atherosclerosis, pharmaceutical companies are racing to produce the next generation of medications to replace the ineffectual ones currently on the market. Niacin, the current drug of choice, increases HDL-C by only 15% to 35%, and then only at daily doses three grams or higher, increasing the chance for unpleasant side effects.

Today at the 33rd annual VEITHsymposiumâ„¢, Dr. Russell H. Sampson, former Associate Professor of Surgery at the Albert Einstein College of Medicine (Bronx, NY) and current President of Mote Vascular Foundation, Inc. (Sarasota, FL), provided a comprehensive overview of the current state of good cholesterol-raising drugs, including two of the more promising ones, Torcetrapib and Rimonabant-Acomplia.

Torcetrapib (discovered and developed by Pfizer), is a cholesteryl ester transfer protein (CETP) inhibitor. In theory, by blocking CETP it should be possible to improve the ratio of HDL-C to low-density lipoprotein cholesterol (LDL-C, also known as "bad" cholesterol), thus slowing the development and progression of atherosclerosis. Early Phase 2 data published in April 2004 showed that inhibiting CETP with torcetrapib at 120 mg per day produced significant increases in HDL-C when given alone (46%), as well as in combination with Lipitor (61%). When the dosage of torcetrapib was increased to 240 mg per day, HDL-C increased by over 100%. However, patients taking 60 mg of torcetrapib with Lipitor also experienced an increase in systolic blood pressure, a drawback which may outweigh the benefit of raised HDL-C. It is currently estimated

that Torcetrapib will be in the U.S. market in 2008.

Rimonabant-Acomplia (discovered and developed by Sanofi-Aventis) is a CB1 endocannabinoid receptor antagonist. CB1 blockers act on the endocannabinoid system, a system controlling energy and nicotine dependence, reducing the overstimulation thought to lead to obesity and nicotine addiction. In a recent study, 1,036 overweight or obese patients with blood lipid disorders were randomly placed in one of three groups (placebo vs. 5 mg or 20 mg per day of Rimonabant-Acomplia). After one year of treatment, patients receiving 20 mg per day of Rimonabant-Acomplia lost an average of 20 pounds, compared to only 5 pounds for patients on placebo. Further comparisons between the placebo and 20 mg per day Rimonabant-Acomplia group showed that the latter patients enjoyed significant improvements in waist circumference and HDL-C and triglyceride levels, all important factors in maintaining heart health. The drug was said to be well tolerated, with only mild and transient side effects like dizziness and gastrointestinal distress. The drug is currently only approved for sale in Europe, with a date for U.S. availability still uncertain.

Dr. Samson said, "We are about to see a whole new generation of medications to help control atherosclerosis the leading cause of death and disability in the USA and most industrial nations. Current medications may halt or slow down progression, however, it is predicted that these medications may revolutionize treatment by actually reversing this disease that is responsible for heart attack, stroke, and amputations. I am extremely excited by the prospect."

About VEITHsymposiumâ„¢

Now entering its fourth decade, VEITHsymposiumâ„¢ provides vascular surgeons, interventional radiologists, interventional cardiologists and other vascular specialists with a unique and exciting format to learn the most current information about what is new and important in the treatment of vascular disease. The 5-day event features 300 rapid-fire presentations from the world's most renowned vascular specialists with emphasis on the latest advances, changing concepts in diagnosis and management, pressing controversies and new techniques.

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PAULINE MAYER
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