Soichi Kumaoka

Studies of plasma levels and urinary excretion after intramuscular injection of triamcinolone acetonide

Abstract Plasma level of triamcinolone acetonide and triamcinolone after the intramuscular injection of 40 mg of triamcinolone acetonide was measured in five patients with advanced breast cancer by adding triamcinolone acetonide-1,2,4- 3 H. The effective level of triamcinolone acetonide continued for 14 to 21 days after the single injection. Plasma level of triamcinolone was significantly lower than triamcinolone acetonide. The suppression of pituitary-adrenocortical function lasted for at least 3 to 4 wk. The urinary excretion of triamcinolone acetonide was low. These results may be due to the high renal threshold and the insoluble feature of this preparation which causes the drug to transmit from the injection site into the blood very slowly, thus allowing triamcinolone acetonide to keep its action over a long period.

Inhibitory effect of mepitiostane on the growth of mammary tumor of a rat.

Mepitiostane (2alpha,3alpha-epithio-5alpha-androstan-17beta-yl 1-methoxycyclopentyl ether) is an orally active anti-estrogenic and anabolic-androgenic steroid compound. Mepitiostane administered orally suppressed the growth of transplanted estrogen-dependent mammary tumor in rats. This result was compared with the oral administration of fluoxymesterone, which is widely used orally for treatment of advanced breast cancer. Experimental result showed that Mepitiostane has a more dominant antitumor activity than fluoxymesterone. Therefore, this new compound may be useful for clinical treatment of breast cancer.