HEXADECYLPHOSPHOCHOLINE - PRECLINICAL AND THE 1ST CLINICAL-RESULTS OF A NEW ANTITUMOR DRUG

被引:55
作者
UNGER, C
EIBL, H
机构
[1] Division of Hematology/Oncology, Department of Internal Medicine, University Hospital Göttingen, Göttingen, D-3400
[2] Max-Planck-Institute for Biophysical Chemistry, Göttingen
关键词
D O I
10.1007/BF02536578
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:1412 / 1417
页数:6
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