Comparison between the in vitro creatinine transport and in vivo serum creatinine elevation on inhibition of renal transporters
| Compound | Total [I]a | Unbound [I] | Quintuple Model IC50 | Unbound [I]/IC50 | Normalized [I]/IC50 (to Cimetidine) | Serum Creatinineb | References |
|---|---|---|---|---|---|---|---|
| μM | μM | μM | μM | ||||
| INCB039110 | ∼3 | ∼1 | 27 | 0.037 | 0.37 | 13 | Incyte unpublished observation |
| Trimethoprim | 5.9 | 3.3 | 80 | 0.041 | 0.41 | 18 | Berglund et al., 1975; FDA BACTRIM drug label |
| Cimetidine | 4 | 3.2 | 32 | 0.10 | 1.0 | 33 | Hilbrands et al., 1991; Somogyi and Gugler, 1983 |