Antineoplastic activity and tolerability of a novel heterocyclic alkylphospholipid, D-20133

Octadecyl-[2-(N-methylpiperidinio)ethyl]-phosphate (OMPEP, D-20133), a heterocyclic analogue of hexadecylphosphocholine (MIL), has been synthesized in an attempt to increase the therapeutic range of the parent compound. The antineoplastic activity of the novel alkylphospholipid was compared with tha...

Full description

Saved in:
Bibliographic Details
Published in:Cancer chemotherapy and pharmacology 1993, Vol.32 (6), p.437-444
Main Authors: STEKAR, J, HILGARD, P, VOEGELI, R, MAURER, H. R, ENGEL, J, KUTSCHER, B, NÖSSNER, G, SCHUMACHER, W
Format: Article
Language:English
Subjects:
9,10-Dimethyl-1,2-benzanthracene
Animals
Antineoplastic agents
Antineoplastic Agents - pharmacology
Antineoplastic Agents - toxicity
Biological and medical sciences
Cell Differentiation - drug effects
Chemotherapy
Female
Ferrets
Mammary Neoplasms, Experimental - chemically induced
Mammary Neoplasms, Experimental - drug therapy
Medical sciences
Pharmacology. Drug treatments
Phosphorylcholine - analogs & derivatives
Phosphorylcholine - pharmacology
Phosphorylcholine - toxicity
Piperidines - pharmacology
Piperidines - toxicity
Rats
Rats, Sprague-Dawley
Tumor Cells, Cultured
Vomiting - chemically induced
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Octadecyl-[2-(N-methylpiperidinio)ethyl]-phosphate (OMPEP, D-20133), a heterocyclic analogue of hexadecylphosphocholine (MIL), has been synthesized in an attempt to increase the therapeutic range of the parent compound. The antineoplastic activity of the novel alkylphospholipid was compared with that of MIL in dimethylbenz(a)anthracene-induced mammary carcinoma of the rat. Using tumors of different sizes and repeated daily doses as well as high single doses, we achieved marked remissions with either compound. However, the therapeutic range of OMPEP was broader than that of the parent drug. Furthermore, the emetic potential of OMPEP tested on ferrets was distinctly less pronounced than that of MIL. In vitro the new alkylphospholipid proved to be more active than MIL in all cell lines tested, and its differentiation-inducing capacity turned out to be superior to that of MIL. No hematological toxicity was observed at various OMPEP doses during a 3-week treatment period.
ISSN:0344-5704
1432-0843
DOI:10.1007/bf00685887