N. Seiler et al., OBSERVATIONS WITH AN S-ADENOSYLMETHIONINE DECARBOXYLASE INHIBITOR IN RATS WITH PROSTATIC ADENOCARCINOMA, Arzneimittel-Forschung, 46(3), 1996, pp. 311-315
CGP 48664A (2-(4-aminoiminomethyl)-2,3-dihydro-1H-1-ylidene, dihydroch
loride, CAS 149400-88-4) is a new potent inhibitor of S-adenosylmethio
nine decarboxylase with antitumor properties. In view of the eminent c
linical problems in the treatment of non hormone dependent prostatic c
ancer, the antiproliferative potency of this compound was tested in Du
nning MAT-LyLu rat prostatic adenocarcinoma. The compound proved ineff
icient in preventing the growth of this tumor, even at a near toxic do
se. A reason for the lacking effect is presumably the inadequate accum
ulation of the drug in the tumor cells due to the excessive growth rat
e of the MAT-LyLu xenografts. Tumor growth seems not to be accompanied
by a proportionally rapid vascularization of the tumor mass. CGP 4866
4A was found to be a potent inhibitor of polyamine oxidase. This prope
rty of the drug may have contributed to the activation of the phagocyt
ic capacity of peritoneal macrophages from tumor-bearing rats.