| 摘要 |
The use of linear alkyl-phosphocholines (I) or (II), containing an acyclic or cyclic ammonio group, in the treatment of benign or malignant tumor diseases, before and/or during treatment with a conventional antitumor agent (A), is new. The use of alkyl-phosphocholines of formula (I) or (II) is claimed in the production of medicaments for the treatment of benign or malignant tumor diseases before and/or during treatment with a conventional antitumor agent (A). [Image] n, m, p, z : 0-4; X : O, S or NH; R : H or 1-20C alkyl (optionally containing 1-3 double and/or triple bonds and optionally substituted by one or more of halo, NO 2, CN, OH, 1-6C alkoxy, NH 2 or mono- or di-(1-4C alkyl)-amino); and R 1-R 3H; or 1-6C alkyl (preferably Me or Et) or 3-7C cycloalkyl (optionally substituted by one or more of halo, NO 2, CN, OH, 1-6C alkoxy, NH 2 or mono- or di-(1-4C alkyl)-amino). An independent claim is included for medicaments, comprising (I) or (II) and optionally carriers and/or auxiliaries, for use as above. ACTIVITY : Cytostatic. Female rats with DMBA-induced mammary cancer were treated on days 0-14 with octadecyl-(1,1-dimethyl-piperidinio-4-yl)-phosphate (IIa) (perifosine; D-21 266) and/or cisplatin (A'), the dose being 14 x 6.81 mg/kg p.o. of (IIa) and/or 4 x 1 mg/kg intraperitoneal of (A'). The tumor weights in various groups were as follows for untreated controls 1.0 g initially and an 875 % increase on day 21, for treatment with (IIa) only 0.9 g initially and a 25 % decrease on day 21, for treatment with (A') only 0.9 g initially and a 410 % increase on day 21, and for treatment with (IIa) plus (A') 0.8 g initially and a 75 % decrease on day 21. MECHANISM OF ACTION : Inositol metabolism modulator; phospholipase interaction modulator; signal transduction modulator. |
