The 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase inhibitors, more commonly known as 'statins', are a novel class of drugs widely used for the treatment of hypercholesterolaemia in patients with established cardiovascular disease as well as those at high risk of developing atherosclerosis. Published chromatographic-mass spectrometric methods for the quantification of presently available seven statins, atorvastatin, simvastatin, lovastatin, pravastatin, fluvastatin, rosuvastatin and pitavastatin are reviewed. High performance liquid chromatography (HPLC) in combination with tandem mass spectrometry (MS/MS) is the analytical technique of choice for the quantification of statins in biological samples. This review envisages that most of the methods used for quantification of statins are in plasma and they are suitable for therapeutic drug monitoring of these drugs.