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Hexadecylphosphocholine: Preclinical and the first clinical results of a new antitumor drug
Author(s) -
Unger Clemens,
Eibl Hansjörg
Publication year - 1991
Publication title -
lipids
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.601
H-Index - 120
eISSN - 1558-9307
pISSN - 0024-4201
DOI - 10.1007/bf02536578
Subject(s) - paclitaxel , pharmacology , alkyl , docetaxel , leukemia , medicine , clinical chemistry , drug , phases of clinical research , phosphocholine , cancer , clinical trial , chemistry , phosphatidylcholine , phospholipid , biochemistry , organic chemistry , membrane
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.