Elevating HDL Cholesterol
Nicotinic acid, taken orally, is the most effective agent to raise HDL cholesterol and to optimize other blood lipids by lowering LDL cholesterol and triglycerides, thereby providing
benefit in the management of risks associated with coronary heart disease and stroke. Niadyne Pharma has developed a topical derivative of nicotinic acid to elevate HDL cholesterol and optimize other blood lipids without the side effects commonly associated with oral nicotinic acid. The scientific and clinical evidence supporting the fact that oral nicotinic acid can effectively raise HDL and lower LDL and triglycerides is well established.
While a major focus of risk management in coronary heart disease and stroke has been to lower LDL and total cholesterol, an equally important goal is to raise HDL. It has been postulated by many scientists that raising HDL may be the most important new preventive action that can be taken to lower risk for heart attack and stroke, as it is responsible for removing the oxidized (damaging) lipids from LDL. However, nicotinic acid, when taken orally in the 1-2 gram dose required for therapeutic effect, has a side effect profile that prevents its widespread use to increase HDL and modify other blood lipids. The major side effect is vasodilation (a redness or flushing of the skin). In addition, high dose oral nicotinic acid
can cause liver damage due to first pass metabolism in the liver.
Dermal delivery of drugs is often preferred as this route of delivery limits first pass metabolism, thus preventing liver damage and
decreasing the dose required for therapeutic effect. For nicotinic acid, the challenge was to find a derivative that could be delivered through the skin without causing flushing, and then be converted into nicotinic acid for rapid delivery into the blood circulation. CARDIO-NIA was designed to diffuse through the skin at a rate that is below the threshold for effecting vasodilation, but once into the skin is rapidly converted to nicotinic acid to achieve a therapeutic effect without side effects.
A recently completed clinical trial has shown our transdermal derivative to be safe and free of side effects including skin flushing. Furthermore, this trial has demonstrated a dose dependent increase in HDL, particularly the cardio-protective HDL3 sub-type, and lowered LDL cholesterol at doses much lower than required for oral nicotinic acid. The use of this agent on a longer-term basis is expected to provide benefits to blood lipids similar to oral nicotinic acid.
