Hypercholesterolemia is considered as one of the most important risk factors and thereby a primary therapeutic target. Measurement of serum lipid concentration helps in identifcation of the subject with cardio metabolic abnormalities or risk of cardiovascular diseases. Although, the benefits of lowering cholesterol level has been widely known for the prevention of heart diseases. AcetylCoenzyme A: cholesterol acyltransferase (ACAT) and cholesteryl ester transfer protein (CETP) are the new targets which are directly or indirectly involved in hyperlipidemia. The rising tide of obesity, diabetes and hypertension are collectively attributed to our reluctance to exercise and desire for fast food. Cessation of smoking, control of blood pressure and blood levels of glucose, low density lipoprotein cholesterol (LDLC), as well as elevation of high density lipoprotein cholesterol (HDLC) levels remain the most effective long-term options for controlling atherosclerosis. Raised Cholesterol Situation and trends in india and globally is described. A variety of drugs used in the therapy belong to the classes of fibrates, statins, bile acid sequestrants, niacin derivatives, as well as, some newer drugs like ezetimibe, avasimibe, eflucimibe, lapaquinstat acetate, lomitapide mesylate, etc., are available in the present antihyperlipidemic therapy, but still there are problems associated with most of these currently available lipid lowering drugs. Current new drug discovery efforts to develop new molecules for antihyperlipidemic research involve focussing on various new molecular mechanisms of hyperlipidaemia and thereby several attractive molecular targets involved thereof in this process are being exploited. Peroxisome proliferation activated receptors (PPARs) [agonists of PPARs] is one of the most important target identified as antihyperlipidemic agents. This review deals with many new molecules may offer an insight for developing new leads for antihyperlipidemic therapy to budding researchers in this field.