Hexadecylphosphocholine, a new ether lipid analogue. Studies on the antineoplastic activity in vitro and in vivo.
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.
Unger
C
C
Department of Internal Medicine, University of Göttingen, West Germany.
Damenz
W
W
Fleer
E A
EA
Kim
D J
DJ
Breiser
A
A
Hilgard
P
P
Engel
J
J
Nagel
G
G
Eibl
H
H
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy; D002794:Choline / Q000031:analogs & derivatives*; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008099:Liver / Q000378:metabolism; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D009364:Neoplasm Recurrence, Local / Q000188:drug therapy; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D011919:Rats, Inbred Strains; D012878:Skin Neoplasms / Q000188:drug therapy / Q000556:secondary; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D010767:Phosphorylcholine; C039128:miltefosine; D002794:Choline