Following oral and i.v. administration of [14 alpha, 15 alpha-3H]-STS 557 to beagle dogs, baboons, rats and female volunteers, plasma level courses of total radioactivity and STS 557, and radioactivity excretion in urine and feces have been investigated. Bioavailability of orally administered STS 557 was found to be 80--90% in man and beagle dog, 70--80% in baboon and rat. Concerning the systemic availability following oral administration of equivalent doses, the following order was established: beagle dog greater than man greater than baboon greater than rat. Equilibrium dialysis indicates species differences in plasma protein binding and a considerable part of STS 557 to be present in plasma unbound. STS 557 is rather rapidly eliminated from the plasma compartment of all species investigated with half lives less than or equal to 10 h. As an additional time parameter of pharmacokinetics the "mean residence time" was used. Urinary excretion of STS 557 metabolites is dominant in all species, including the rat. In contrast to the great part of STS 557 in plasma total radioactivity, only small amounts of unchanged STS 557 are excreted in urine. First results of current studies in rabbits are presented, too.
The kinetics of xenobiotic biotransformation was measured in single, isolated, perifused liver cells with microspectrofluorometry using highly sensitive photodetection systems. A program of further applications to biochemical toxicological problems is presented.
The present investigation has analyzed 249 patients suffering from urogenital cancer in respect to aberrant concentration of prolactin, TSH, LH and FSH. A simultaneous pattern of acute phase reactants (α1 glycoprotein, α1-antitrypsin, β2-glycoprotein and haptoglobin) was related to the content of these hormones. Abnormal results of prolactin and TSH were present in 30% of all patients, whereas frequent aberrations of α1-acid glycoprotein and α1-antitrypsin were detected in 60–80%. Acute phase reactants changed to more pathological values when correlated to elevated prolactin.
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