Background: Hyperlipidemia is characterized by high level of cholesterol and triglycerides
in blood. Various classes of drugs like statins, fibrates, niacin etc. are used for treatment of
Objective: Niacin, which is one of the beneficial anti-hyperlipidemic agents, helps decreasing LDL
cholesterol by 20 to 40% and causes increase of HDL cholesterol by 20 to 35%. However cutaneous
flushing, loss of glucose tolerance, liver toxicity are the reported side effects of niacin therapy responsible
for decreased patient compliance. Very recently, the G protein coupled receptor (GPCR);
GPR109A located on the adipocytes has been identified as the receptor for activation of niacin.
Method: In-vitro studies have demonstrated that GPR109A receptor having high affinity for niacin.
The present review attempts to provide a systematic presentation of the various chemical classes of
compounds that have been reported as novel niacin receptor agonists including pyrazole-3-carboxylic
acids, urea derivatives, anthranilic acids, biaryl anthranilides, tetrahydro anthranilic acid, xanthines,
barbituric acid, bicyclic pyrazole carboxylic acids, pyrido pyrimidinones, pyrazolyl propionyl cyclohexenamides,
pyrazole acids etc.
Results: As the design of GPR109A receptor agonists offers a promising solution for treatment of
dyslipidemia, this review will be beneficial for medicinal and drug discovery chemists to expediate
the process of discovery of new class of anti-hyperlipidemic agent with favorable lipid lowering profile
with increase in HDL levels.
Conclusion: This review explains novel GPR109A receptor agonists for the treatment of dyslipidemia.