Table 5.

Activity of lonaprisan, vilaprisan, and their metabolites in the in vitro transactivation assay and the percentage of AUC(0–∞) of their metabolites in human plasma.

Compound	PR transactivation assay IC50 [nm]	% AUC of parent
lonaprisan	0.02	N/A
1	0.14	285[a]
2	0.10	312[a]
3	3.3	920[a]
18 (vilaprisan)	0.09	N/A
20	5.3	24[b]
21	610	19[b]

[a] Determined by LC–MS after single oral administration of 200 mg lonaprisan to humans. [b] Determined by LC–MS after multiple oral administration of 5 mg day⁻¹ vilaprisan.