Plasma and liver concentrations of GEM and its metabolites and their estimated inhibitory effects on the elimination of CER in the liver in clinical situationsa
GEM | GEM-1-O-glu | |
|---|---|---|
| Cmaxb (μM) | 100-150 | 20 |
| 1+I/IC50_OATP2 | 2.4-3.1 | 1.8 |
| 1+I/IC50_metabolism | 2.2-2.6 | 2.2 |
| Cmax,uc (μM) | 0.65-0.97 | 2.3 |
| 1+I/IC50_OATP2 | 1.0 | 1.1 |
| 1+I/IC50_metabolism | 1.0 | 1.3 |
| Cmax,u,liverd (μM) | 81-97 | |
| 1+I/IC50_metabolism |
| 3.1-3.2 |
↵ a Inhibitory effects of GEM and GEM-1-O-glu are represented by 1 + inhibitor concentration (I)/IC50.
↵ b Plasma concentrations of GEM and GEM-1-O-glu are reported by Backman et al. (2002) and Okerholm et al. (1976).
↵ c Plasma unbound concentrations.
↵ d Estimated unbound concentrations in the liver.