Endometriosis is a chronic, mainly estrogen-dependent disease characterized by the presence of endometrial tissue outside the uterus in the peritoneal cavity. Aldo-keto reductase 1C3 (AKR1C3/ 17β-hydroxysteroid dehydrogenase type 5) is an enzyme, combining 17β-hydroxysteroid dehydrogenase and prostaglandin (PG) F synthase activity. AKR1C3 has been described to play a crucial role in intra-tissue steroid and prostaglandin metabolism. Expression of the enzyme in lesions is expected to lead to increased local concentrations of steroid hormones (especially estradiol) and of PGF2α. This pro-estrogenic environment with increased PGF2α concentration is thought to stimulate proliferation and growth of estrogen-sensitive endometriotic lesions. To demonstrate the role of AKR1C3 in endometriosis, the novel and selective AKR1C3 inhibitor BAY 1128688 was identified and tested in a marmoset monkey endometriosis model. The identification of BAY 1128688, which is currently in clinical trials, will be presented. Moreover, SAR aspects and research data related to the new compound class will be reported.

First time disclosure of BAY 1128688: A novel AKR1C3 inhibitor for the treatment of endometriosis

254th National Meeting (2017)

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