BAY-1128688 is a potent, orally active and selective AKR1C3 inhibitor with IC50 < 2 nM. BAY-1128688 shows high selectivity over related AKR1C enzymes (1C1, 1C2, 1C4) and AKR1D1. BAY-1128688 exhibits no relevant activity at major nuclear hormone receptors. BAY-1128688 reduces endometriotic lesions in the marmoset monkey endometriosis model. BAY-1128688 can be used for endometriosis research [1].
References:
[1]. Hilpert J, et al. Hepatotoxicity of AKR1C3 Inhibitor BAY1128688: Findings from an Early Terminated Phase IIa Trial for the Treatment of Endometriosis. Drugs R D. 2023 Sep;23(3):221-237.
References:
[1]. Hilpert J, et al. Hepatotoxicity of AKR1C3 Inhibitor BAY1128688: Findings from an Early Terminated Phase IIa Trial for the Treatment of Endometriosis. Drugs R D. 2023 Sep;23(3):221-237.