The in vivo metabolism of tibolone in animal species

@article{Verhoeven2010TheIV,
  title={The in vivo metabolism of tibolone in animal species},
  author={C. Verhoeven and R. Vos and L. Delbressine},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
  year={2010},
  volume={27},
  pages={1-10}
}
SummaryThein vivo tissue distribution and metabolism of tibolone was studied in different animals to further investigate the compound’s tissue-specificity. Tibolone’s metabolism was studiedin vivo in rats and rabbits by administration of [16-3H]-tibolone and the metabolic pattern was determined in urine and faeces after oral administration to female rats and dogs.The main excretory pathway was found to be excretion in the faeces. Important phase-I metabolic routes were the reduction of the 3… Expand
Pharmacokinetics, Tissue Distribution and Excretion of Verticinone from F. hupehensis in Rats
TLDR
A significant gender difference in the pharmacokinetics of verticinone in rats was observed, as its absolute oral bioavailability in male and female rats was 45.8% and 2.74%, respectively. Expand
A Review of Analytical Methods for the Determination of Tibolone: Pharmacokinetics and Pharmaceutical Formulations Analysis and Application in Doping Control
Tibolone is a synthetic steroid commercialized by Organon under the brand name Livial (Org OD14), which is used in hormone therapy for menopause management and treatment of postmenopausalExpand
Bioequivalence Studies of Tibolone in Premenopausal Women and Effects on Expression of the Tibolone‐Metabolizing Enzyme AKR1C (Aldo‐Keto Reductase) Family Caused by Estradiol
TLDR
The authors did not find significant differences in pharmacokinetic parameters between the 2 formulations, but metabolite formation was different from reports in postmenopausal women, which might result from changes in AKR1C family expression by patient estrogen status. Expand
Effect of tibolone pretreatment on kinases and phosphatases that regulate the expression and phosphorylation of Tau in the hippocampus of rats exposed to ozone
TLDR
It is observed that O3 exposure increases Tau phosphorylation, which is correlated with decreased PP2A and PTENprotein levels, diminished Akt protein levels, and increased GSK3β protein levels in the hippocampus of adult male rats. Expand
Tibolone facilitates lordosis behavior through estrogen, progestin, and GnRH-1 receptors in estrogen-primed rats
TLDR
The results suggest that TBL stimulates lordosis by activating estrogen, progesterone, and may do so by downstream stimulation of GnRH release and may be influenced by the physiological role TBL plays in controlling lordosis behavior. Expand
Tibolone: the way to beat many a postmenopausal ailments
TLDR
Clinical trials prove that tibolone is effective in the treatment of the menopausal symptoms and for the postponement and calming of symptoms accompanying age-related diseases. Expand
Application of UPLC–MS/MS for separation and quantification of 3α-Hydroxy Tibolone and comparative bioavailability of two Tibolone formulations in healthy volunteers
TLDR
It is concluded that test formulation of Tibolone is bioequivalent to reference formulation of TsI, and this method was successfully applied to a pharmacokinetic study in 50 post-menopausal/surgical menopause female human volunteers under fasting conditions. Expand
Tibolone induces lordosis behavior, but not concurrent or sequential inhibition, in Sprague Dawley rats
TLDR
TBL likely induces its facilitation of lordosis by an action that is independent of PR, and unlike P, TBL did not induce CI or SI. Expand
Regain d’intérêt pour la grenade, un fruit majestueux aux multiples propriétés
TLDR
Pomegranate is proposed as an adjunct in the treatment of certain diseases such as cardiovascular disease, diabetes and some cancers particularly that of the prostate, which has found an unprecedented upsurge of interest among both scientists and consumers. Expand

References

SHOWING 1-10 OF 23 REFERENCES
In vitro and in vivo metabolism of the progestagen Org 30659 in several species.
TLDR
The metabolism of Org 30659, a new potent progestagen currently under clinical development by NV Organon for use in oral contraceptive and hormone replacement therapy, was studied in vivo after oral administration to rats and monkeys and in vitro using rat, rabbit, monkey, and human liver microsomes and rat and human hepatocytes. Expand
In vitro and in vivo metabolism of desogestrel in several species.
TLDR
The metabolism of desogestrel, an orally active progestogen, was studied in vivo after administration of single oral doses to rats and dogs and in vitro using rat, rabbit, dog, and human liver microsomes to identify metabolites. Expand
Metabolism of three pharmacologically active drugs in isolated human and rat hepatocytes: analysis of interspecies variability and comparison with metabolism in vivo.
TLDR
The reflection of interspecies differences in isolated hepatocytes, with respect to both metabolite profiles and human-specific metabolites, renders isolated human hepatocytes a very valuable tool during preclinical drug development. Expand
Indomethacin-sensitive 3α-hydroxysteroid dehydrogenase in rat tissues
The purified 3α-hydroxysteroid dehydrogenase (EC 1.1.1.50) of rat liver cytosol is potently inhibited by the nonsteroidal anti-inflammatory drugs in rank-order of their therapeutic potency, i.e. byExpand
Purification and properties of human hepatic 3α-hydroxysteroid dehydrogenase
Abstract 3α-Hydroxysteroid dehydrogenase (3α-HSD) was purified greater than 500-fold from human liver cytosol. The purification was monitored using 5β-[ 3 H]dihydrocortisol (5β-DHF) as substrate.Expand
Partial characterization of the cytosol 3 alpha-hydroxysteroid: NAD(P)+oxidoreductase of rat ventral prostate.
TLDR
The cytosol 3alpha-hydroxysteroid dehydrogenase of rat ventral prostate has been partially purified and conclusions have been drawn that many delta4,3-keto steroids that cannot act as substrates for the enzyme inhibit the enzyme competitively and may well serve as physiological regulators of the reaction in intact cell. Expand
Molecular structure of rat hepatic 3 alpha-hydroxysteroid dehydrogenase. A member of the oxidoreductase gene family.
TLDR
The significant homology of 3 alpha-HSD with both prostaglandin F synthetase and aldose reductases suggest a subdivision of monomeric, NADPH reductase within the larger oxidoreductases superfamily. Expand
Clinical profile of Org OD 14.
TLDR
It was concluded that Org OD 14 is an effective and safe new preparation for the treatment of climacteric patients and had a beneficial effect on mood and libido. Expand
Affinity labeling of human placental 3 beta-hydroxy-delta 5-steroid dehydrogenase and steroid delta-isomerase: evidence for bifunctional catalysis by a different conformation of the same protein for each enzyme activity.
TLDR
Analysis of the ligand-induced conformational change along with cofactor protection data suggests that the enzyme expresses both activities at a bifunctional catalytic site, which explains a shift from a dehydrogenase to an isomerase conformation in response to rising secosteroid levels. Expand
Endocrinological studies with (7 alpha, 17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14).
A novel steroid, (7 alpha, 17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14), is described which has concomitant weak estrogenic, progestational and androgenic activities.Expand
...
1
2
3
...