1. Alkyllyso-derivatives of physiologic cell membrane phospholipids show remarkable cytostatic and cytotoxic activity on many malignant tumor cell lines and tumors in vitro and in vivo. Three of these etherphospholipid analogues have already been tested in clinical phase II studies and one of these compounds, hexadecylphosphocholine (HePC), is now commercially available as a drug for the treatment of mammary carcinoma in Germany. 2. Etherphospholipid analogues possess a variety of interesting biological characteristics like induction of cellular maturation, inhibition of tumor cell invasion or modulation of the immune response with high potential value for tumor therapy. 3. Though there have been extensive investigations on the biochemical mode of action of these substances, the precise mechanism responsible for the majority of biological effects has not yet been identified. 4. In recent years growing evidence has been accumulated that etherphospholipid analogues substantially interfere with intracellular signal transduction.