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. 2018 Nov 8;13(21):2271–2280. doi: 10.1002/cmdc.201800487

Table 1.

In vitro activity and metabolic stability in liver microsomes of lonaprisan and its human metabolites.

graphic file with name CMDC-13-2271-g007.jpg
Compound Y PR transactivation assay Metabolic stability assay
    IC50 [nm][a] Efficacy [%] F max Human [%][a] F max Rat [%][a]
lonaprisan graphic file with name CMDC-13-2271-g008.jpg 0.02 100 77 83
metabolite 1 graphic file with name CMDC-13-2271-g009.jpg 0.14 100 58 81
metabolite 2 graphic file with name CMDC-13-2271-g010.jpg 0.10 100 50 57
metabolite 3 graphic file with name CMDC-13-2271-g011.jpg 3.3 100 68 82

[a] Concentration of drug resulting in 50 % inhibition. [b] Maximum oral bioavailability calculated from in vitro hepatic extraction ratio (E H) in liver microsomes, assuming 100 % absorption (F max=1−E H); see the Experimental Section for details.