TABLE 1

In vivo pharmacokinetic parameters of OMP and its metabolites

f_u,p is the fraction of OMP and metabolites unbound in plasma, AUC_m is the AUC of the metabolite, AUC_p is the AUC of the parent (OMP), and AUC_t is the summed AUC of all measured compounds.

Inhibitor	Clog P	C_max	AUC_0-∞	f_u,p	AUC_m/AUC_p		AUC_m/AUC_t^{^a}
Inhibitor	Clog P	C_max	AUC_0-∞	f_u,p	Total AUC_0-∞	Unbound AUC_0-∞	Total AUC_0-∞
		µM	hrnM*
OMP	2.23	0.66 ± 0.34	1200 ± 600	0.05 ± 0.02
OH-OMP	0.98	0.48 ± 0.33	1000 ± 400	0.17 ± 0.03	0.83	2.7	≤ 0.27
DM-OMP	1.90	0.03 ± 0.01	49 ± 12	1.0 ± 0.1	0.04	0.79	≤ 0.01
OMP-S	2.24	0.14 ± 0.10	390 ± 220	0.02 ± 0.004	0.33	0.14	≤ 0.10
C-OMP	1.39	0.25 ± 0.10	1100 ± 400	0.08 ± 0.02	0.92	1.4	≤ 0.29

↵^a In the absence of a mass-balance study, the maximum possible fraction of total drug-related material was estimated as a fraction of all quantified compounds.