1. Field
This application relates to the treatment of hypertriglyceridemia and reducing the risk of developing this condition.
2. Background Information
A triglyceride is an ester derived from glycerol and three fatty acids. Triglycerides are the main lipid component of dietary fat and fat depots of animals. Triglycerides are transferred via the blood between tissues, e.g., between adipose tissue and liver tissue, by lipoprotein particles. The highest triglyceride concentrations are found in chylomicrons and very low density lipoprotein particles.
The American Heart Association classifies individuals by their fasting serum triglyceride levels as follows: <150 mg/dL, normal; 150 to 199 mg/dL, borderline high; 200 to 499 mg/dL, high; and ≧500 mg/dL, very high. Elevated triglyceride levels, known as hypertriglyceridemia, contribute to the development of atherosclerosis, cardiovascular disease, and acute pancreatitis.
Most often, hypertriglyceridemia is caused by obesity, lipodystrophic disorders, diabetes mellitus, metabolic syndrome, and chronic kidney disease. In some instances, it can be caused by familial genetic disorders.
Typically, life-style modifications are recommended for individuals having borderline high triglyceride levels (150 to 199 mg/dL). Lifestyle modifications encompass changes in diet, exercise, weight reduction, smoking cessation, and limiting alcohol intake. Optimization of nutrition can result in a marked reduction in serum triglycerides by as much as 20% to 50%.
Patients with levels of triglycerides greater than 200 mg/dL are prescribed lipid-lowering drugs. The major pharmacological treatment options for hypertriglyceridemia are HMG-CoA reductase inhibitors (e.g., atorvastatin, fluvastatin, pitavastatin, pravastatin, lovastatin, simvastatin, and rosuvastatin), fibric acid derivatives (e.g., gemfibrozil and fenofibrate), nicotinic acid (niacin), cholesterol absorption inhibitors, bile acid sequestrates (resins), and ω-3-acid ethyl esters.
Current pharmacological treatments for hypertriglyceridemia do not effectively control high triglyceride levels without unfavorable adverse effects. The need exists for efficient treatments for hypertriglyceridemia that have fewer side effects.