Hexadecylphosphocholine, better known as miltefosine, belongs to the group of phospholipids. The long alkyl chain and a polar group of a molecule proved to be essential for antitumor activity, especially to cure breast cancer cells. The apoptotic process takes place in the plasma membrane, where molecules are inserted and then influence signaling pathways. Moreover, during preclinical studies hexadecylphosphocholine (He-PC) found to be highly effective in inhibiting the growth of chemically induced rat mammary carcinomas, and even a high percentage of the tumors regressed completely. The He-PC has many more applications such as antifungal agent, antiprotozoal drug, protein kinase inhibitor or immunomodulator. Even though miltefosine was originally developed in the 1980s as an anti-cancer agent, new studies have demonstrated activity against Leishmania parasites and neoplastic cells, and due to broad spectrum of antimicrobial effects, it is recommended as a first line treatment for free-living amebae infections.