STEAR
Stear ( English selective tissue estrogenic activity regulator ) are agents that act through estrogen receptors mediate and a selective affinity have to certain tissues. The first member of this class to be used as a medicinal product is the steroid tibolone . Tibolone only becomes active after it has been metabolized. The estrogenically active 3-hydroxytibolone, which is formed, among other things, by hydroxylation in position 3, is converted into ineffective, sulfated substances in most tissues by sulfotransferases occurring there . In contrast, there are only a few sulfotransferases in the bone tissue, but more sulphatases, which hydrolytically convert the conjugates back into active metabolites. The breakdown of bone is inhibited. Tibolone is used to treat symptoms of estrogen deficiency in postmenopausal women.
swell
- ↑ Ernst Mutschler: Mutschler drug effects. Pharmacology, clinical pharmacology, toxicology. 10th edition. Stuttgart 2013, p. 418.