Lysophosphatidylcholine (LPC) is a major plasma lipid that has been recognized as an important cell signalling molecule produced under physiological conditions by the action of phospholipase A(2) on phosphatidylcholine. LPC transports glycerophospholipid components such as fatty acids, phosphatidylglycerol and choline between tissues. LPC is a ligand for specific G protein-coupled signalling receptors and activates several second messengers. LPC is also a major phospholipid component of oxidized low-density lipoproteins (Ox-LDL) and is implicated as a critical factor in the atherogenic activity of Ox-LDL. Hence, LPC plays an important role in atherosclerosis and acute and chronic inflammation. In this review we focus in some detail on LPC function, biochemical pathways, sources and signal-transduction system. Moreover, we outline the detection of LPC by mass spectrometry which is currently the best method for accurate and simultaneous analysis of each individual LPC species and reveal the pathophysiological implication of LPC which makes it an interesting target for biomarker and drug development regarding atherosclerosis and cardiovascular disorders.