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See the DrugPatentWatch profile for niacin
How do non-statin drugs like niacin work compared to statins? Niacin lowers LDL cholesterol and raises HDL by slowing liver fat production and limiting how much the liver releases VLDL particles. It does this durch blocking DGAT2, DGAT2 is a enzyme that helps assemble VLDL. It also activates GPR109A, a receptor on fat cells that stops fat breakdown and reduces free fatty acids sent to the liver. Different from statins, niacin does not block HMG-CoA reductase, which is the main mechanism of statins. What clinical data shows about niacin’s effectiveness? Early studies showed niacin alone or with statins reduced cardiovascular events. Early studies showed 15–25 % LDL reduction and 15–35 % HDL increase. Recent large trials, however, showed no cardiovascular benefit and added risks. The AIM-HIGH and HPS2-THRIVE trials both stopped early because niacin did not cut heart attacks or strokes beyond statin therapy alone. What side effects are patients asking about? Patients commonly report flushing, itching, and gastrointestinal discomfort. Flushing occurs because niacin activates GPR109A on skin cells, causing prostaglandin release. The flushing can can be reduced by taking aspirin 30 minutes before niacin or by using extended-release forms. When does the niacin patent expire? Niacin has been available since 1955 and is generic. No new patents protect the basic molecule itself. Extended-release formulations such as Niaspan had patents that expired in 2011.
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