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Hexadecylphosphocholine: Preclinical and the first clinical results of a new antitumor drug

  • Alkyl Lysophospholipids in Cancer Therapy
  • Review
  • Published:
Lipids

Abstract

Dose-response studies on cytotoxic alkyl lysophospholipids with various chemical structures revealed that a long alkyl chain and a polar group are essential for antitumor activity. The combination of both the long alkyl chain and a phosphocholine group thus results in alkyl phosphocholines. Preclinical, studies with hexadecylphosphocholine (He-PC) as a representative compound indicate distinct antineoplastic activity on leukemia cells of human origin. He-PC is highly effective in inhibiting the growth of chemically induced rat mammary carcinomas. Even more striking is the fact that a high percentage of the tumors regressed completely. In a clinical phase I trial on breast cancer patients with local recurrences, topically applied He-PC resulted in regression of skin metastases. A phase II trial for topical treatment and a phase I trial for orally applied He-PC have been initiated to further evaluate the antitumoral activity of this new compound.

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Abbreviations

ALP:

alkyl lysophospholipids

CMC:

criticl micelle concentration

DMBA:

7,12-dimethylbenzanthracene

ET-18-OCH3 :

1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine

G-3-PC:

glycero-3-phosphocholine

GM-CSF:

granulocyle macrophage-colony stimulating factor

He-PC:

hexadecyl phosphocholine

ID50 :

50% inhibition dosage

LD50 :

half lethal dosage

Log p:

oil/water partition coefficient

MNU:

methylnitrosourea

PAF:

1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine

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Authors and Affiliations

  1. Max-Planck-Institute for Biophysical Chemistry, D-3400, Göttingen, Federal Republic of Germany

    Hansjörg Eibl

  2. Division of Hematology/Oncology, Department of Internal Medicine, University Hospital Göttingen, Robert-Koch-Str. 40, D-3400, Göttingen, Federal Republic of Germany

    Clemens Unger

Authors
  1. Clemens Unger
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  2. Hansjörg Eibl
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Unger, C., Eibl, H. Hexadecylphosphocholine: Preclinical and the first clinical results of a new antitumor drug. Lipids 26, 1412–1417 (1991). https://doi.org/10.1007/BF02536578

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  • DOI: https://doi.org/10.1007/BF02536578

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