Hexadecylphosphocholine, a new ether lipid analogue. Studies on the antineoplastic activity in vitro and in vivo

Acta Oncol. 1989;28(2):213-7. doi: 10.3109/02841868909111249.

Abstract

Hexadecylphosphocholine (He-PC) is a new compound synthesized according to the minimal structural requirements deducted from studies with other ether lipids. In vitro studies on He-PC revealed remarkable antineoplastic activity on HL60, U937, Raji and K562 leukemia cell lines. In addition, He-PC, applied orally, showed a superior effect in the treatment of dimethylbenzanthracene-induced rat mammary carcinomas when compared to intravenously administered cyclophosphamide. After oral application He-PC was well absorbed from the intestine and metabolized in the liver by phospholipases C and D. During a 5-week treatment no hematotoxic effects were detected. In a clinical pilot study on breast cancer patients with widespread skin involvement, topically applied He-PC showed skin tumor regressions without local or systemic side effects.

MeSH terms

  • Animals
  • Antineoplastic Agents* / metabolism
  • Antineoplastic Agents* / therapeutic use
  • Breast Neoplasms / drug therapy
  • Choline / analogs & derivatives*
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Liver / metabolism
  • Mammary Neoplasms, Experimental / drug therapy
  • Mice
  • Neoplasm Recurrence, Local / drug therapy
  • Phosphorylcholine / analogs & derivatives*
  • Phosphorylcholine / metabolism
  • Phosphorylcholine / pharmacology
  • Phosphorylcholine / therapeutic use
  • Rats
  • Rats, Inbred Strains
  • Skin Neoplasms / drug therapy
  • Skin Neoplasms / secondary
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Phosphorylcholine
  • miltefosine
  • Choline