Tibolone metabolism in human liver is catalyzed by 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four isoforms of the aldo-keto reductase (AKR)1C subfamily.

@article{Steckelbroeck2006TiboloneMI,
  title={Tibolone metabolism in human liver is catalyzed by 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four isoforms of the aldo-keto reductase (AKR)1C subfamily.},
  author={Stephan Steckelbroeck and Busola Oyesanmi and Yi Jin and S Lee and Helenius J. Kloosterboer and Trevor M Penning},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2006},
  volume={316 3},
  pages={1300-9}
}
Tibolone [[7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one] is used to treat climacteric symptoms and prevent osteoporosis. It exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a Delta4-isomer. Recombinant human cytosolic aldo-keto reductases 1C1 and 1C2 (AKR1C1 and AKR1C2… CONTINUE READING