Hexadecylphosphocholine: preclinical and the first clinical results of a new antitumor drug.
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.
Unger
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Department of Internal Medicine, University Hospital Göttingen, Federal Republic of Germany.
Eibl
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D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008875:Middle Aged; D009369:Neoplasms / Q000188:drug therapy*; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
D000970:Antineoplastic Agents; D010767:Phosphorylcholine; C039128:miltefosine