Uptake and metabolism of estramustine in the Dunning R3327H tumour
1Department of Biochemistry, University of Lund, Sweden.
Abstract:
A time-dependent plasma, tumour cell and nuclear uptake was found after intraperitoneal 3H-estramustine administration, in rats bearing the Dunning H tumour. Uptake of the drug into tumour cells had not reached a maximum after 4 h, whereas no real change was seen in the nuclear fraction after 2 h. Binding to the nuclear protein matrix of Dunning H tumour cells of 3H-estramustine was also found (2.46 pmol/g protein). High performance liquid chromatography demonstrated the existence of estramustine, its oxidized metabolite estromustine, estradiol and estrone in the plasma and the tumour after intravenous administration of 100 microCi 3H-estramustine.
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