Biochemistry of drugs. XXIV. Substances with antineoplastic effect. LXII. Pharmacokinetics of gamma,gamma-bis-4-ethylphenyl-alpha,beta-dibromoisocrotonic acid-3H (Edikron-3H) in experimental animals.

ABSTRACT

After oral administration of Edikron-3H to mice with mammary gland adenocarcinoma HK, within 24 h after ingestion almost 50% of administered radioactivity was excreted (16% in urine, 33% in faeces), and within 4 day it was almost 80% (27% in urine, 50% in faeces). Like in mice, also in dogs the faecal excretion preponderated. In mice, the levels in most tissues and blood culminated at hour 6 after administration of the substance. Relatively high levels were found in the liver, the levels in other tissues and blood being substantially lower in comparison. The levels in the tumor were initially low, later on they rose, and culminated at hour 24. Besides, it was found that the transfer of radioactivity by milk into the sucklings' bodies was relatively low, and radioactivity penetration into fetuses was negligible. In urine, unchanged parent substance was present in very slight amounts only.