Hypercholesterolemia is one of the main factors in the development of atherosclerotic
cardiovascular disease. The advent of
statins led to huge progress in the treatment of
hypercholesterolemia, yet the proportion of patients with prohibitive
lipid values and the high incidence of cardiovascular events despite treatment are still very high.
Niacin, one of the older drugs used to treat
hyperlipidemia, was shown to reduce
low-density lipoprotein-cholesterol (
LDL-C) and
triglycerides and to markedly increase
high-density lipoprotein-cholesterol (HDL-C) levels. This
drug came into disuse owing to frequent side effects, mainly
flushing, but in recent years a reemergence of its application has occurred, and multiple clinical trials have shown its effectiveness in the treatment of
hyperlipidemia and in the reduction of cardiovascular events. New formulations such as extended-release
niacin (ERN) have been developed with the purpose of reducing side effects. Lately, a new compound,
laropiprant, which selectively antagonizes the
prostaglandin 2 (
PGD2) receptor responsible for
flushing, has been developed.
Laropiprant, when combined with ERN, significantly reduces the incidence of
flushing. New and ongoing trials will definitively prove in the long term whether this
drug combination significantly reduces the severity of
flushing and the incidence of cardiovascular events.