The concentration of lysophospholipids (LPL) increases under pathological conditions and, thus, LPL attract diagnostic and pharmacological interest. LPL are particularly interesting because they possess pro- and anti-inflammatory properties and can be generated by phospholipases and reactive oxygen species (ROS). This review provides an overview of the mechanisms by which LPL are generated and how they can be determined. The effects of LPL as signaling molecules and their roles in different pathologies are discussed. The focus will be on lysophosphatidylcholine (LPC).