Cordaptive: Niacin Without The Side Effects
Cordaptive is a combination drug consisting of one gram of extended-release nicotinic acid and laropiprant, a drug designed to reduce the flushing, rash, and other side effects associated with niacin use. Nicotinic acid affects all aspects of your lipid profile, raising HDL levels by between 15 to 30%, as well as lowering LDL levels by 15 to 25% and triglycerides levels by 20 to 50%.This drug combination is unique among other extended release niacin products because it is the only one on the market that includes a component to reduce the side effects experienced with niacin.
Laropiprant targets a molecule, prostaglandin D2 subtype 1, that causes vessels to be dilated when niacin is taken. This vessel dilation is what is thought to be responsible for the flushing and other undesirable side effects associated with taking niacin. And, according to current studies, the laropiprant and niacin combination causes less flushing than taking niacin by itself.
Cordaptive is manufactured by Merck, but this drug is not available by prescription yet. Merck has gained approval by the Food and Drug Administration to manufacture the drug, and has submitted an application to distribute Cordaptive in the United States.
This drug may be used alone; however, Merck is also planning to market this drug with the cholesterol-lowering drug Zocor (simvastatin). Coincidently, Abbot has also began manufacturing its new drug, Simcor, which is a combination of its own brand of extended release nicotinic acid (Niaspan) and Zocor.
Does Cordaptive Work?
Current studies involving Cordaptive appear promising. Over 1,600 individuals with high cholesterol taking the drug (extended release nicotinic acid 1 g and laropiprant 20mg) alone experienced a 17% decrease in LDL, a 22% decrease in their triglycerides, and a 23% increase in HDL.When Zocor was combined with Cordaptive, an even larger improvement was noted in the cholesterol profile of the individuals participating in this study. While HDL was raised by 28% and triglycerides were lowered by 33%, LDL was lowered by almost 48%. This is a marked reduction in cholesterol in comparison to taking Cordaptive alone.
However, it should also be noted that, during this phase of the study, the participants were started out on Zocor 10 mg or 40mg and a nicotinic acid dose of 1 g for the first four weeks, and their dose of nicotinic acid was increased to 2 g for eight weeks until the conclusion of the study. So, in order to truly compare the effects of a Zocor/Cordaptive combination to Cordaptive alone, we would need to have consistent doses of Cordaptive present.
Side Effects and Cordaptive
The major side effect noted in the study so far was the flushing effect experienced with nicotinic acid. Roughly 4.8% of individuals participating in the study had to discontinue the Zocor/Cordaptive combination due to flushing, whereas the 8.7% of participants only taking Cordaptive stopped taking the drug due to the niacin-induced side effects. However, it is important to note that while flushing was still present in these patients, the incidence of experiencing flushing while on niacin alone would likely be much higher.Significantly raised liver enzymes were only seen in 0.3% of individuals taking the Zocor/Cordaptive combination and 0.5% of individuals only taking Cordaptive. The participants experiencing this increase were asymptomatic and had their liver enzymes return to normal once the drug was discontinued.
Additionally, blood glucose levels were slightly increased in some participants. This is another known side effect of niacin. There were also no cases of myopathy or hepatitis reported in these individuals, which are rare occurrences in individuals taking statins, high doses of nicotinic acid, or both of these products together.
Sources:
Lai E, De Lepeleire I, Crumley TM. Suppression of niacin-induced vasodilation with an antagonist to prostaglandin D2 receptor subtype 1. Clin Pharmacol Ther. 2007 Jun;81(6):849-57.
Merck Official Website. 2007. http://www.merck.com/newsroom/press_releases/research_and_development/2007_1105.html. Available at: Accessed 10 November 2007.
Merck Official Website. 2007. http://www.merck.com/newsroom/press_releases/research_and_development/2007_0902.html. Available at: Accessed 10 November 2007.
Third Report of the National Cholesterol Education Program
(NCEP) Expert Panel on Detection, Evaluation, and Treatment of
High Blood Cholesterol in Adults (PDF), July 2004, The National Institutes of Heath: The National Heart, Lung, and Blood Institute.
