DROXYPHENYL)ETHYLENEDIAMINE]-DICHLOROPLATINUM(II), A NEW DRUG NOT ONLY PARENTERALLY BUT ALSO ORALLY-ACTIVE IN THE THERAPY OF BREAST AND PROSTATE-CANCER

The platinum complex droxyphenyl)-ethylenediamine]dichloroplatinum(II) , K, was tested for its antitumor activity on hormone-sensitive tumor models under peroral administration. The resorption from the gastroint estinal tract was proved by determining the estrogenic effect of K in a dose/activity study using the immature-mouse uterine weight test. In comparison to the subcutaneous injection, a tenfold peroral dose was administered to achieve identical effects. By peroral treatment of the hormone-sensitive MXT(M3.2) mammary carcinoma of the mouse with K an almost complete inhibition of the tumor growth was obtained. This effe ct was superior to that of subcutaneously applied cisplatin and signif icantly better than that obtained by perorally administered ligand L a t an equimolar dose, indicating that the antitumor effect is caused by the intact complex K and not by the liberated ligand L. The strong an titumor activity of perorally applied K was also demonstrated on the h ormone-sensitive Noble Nb-R prostatic carcinoma of the rat. Histologic al examinations showed that the platinum complex K did not cause cispl atin-like kidney damage or irritations of gastric or intestinal mucosa when given perorally.