Values used for IVIVE of metformin CLr,sec
| Human in vivo CLr,sec of metformin: geometric mean (range) 415 (215–643) ml/min | HEK293 | MDCKII |
|---|---|---|
| Human kidney weight (g) | 150 | 150 |
| Cortex weight/kidney (70% of total kidney weight) (g)a | 105 | 105 |
| OCT2 expression in cells (pmol/mg protein) | 369.4 | 19 |
| OCT2 expression in kidney cortex (pmol/mg protein) | 7.6 | 7.6 |
| In vitro metformin clearance (µl/mg protein per minute) | 36.7 ± 2.8 | 2.0 ± 0.1 |
| Scaling factor (SF): [E]in vivo/[E]in vitro | 0.02 | 0.40 |
| Milligrams of protein per milligram human kidney cortex weightb | 0.3 | 0.3 |
| [14C]-metformin uptake (pmol/min per milligram protein)b | 202.1 ± 15.6 | 10.9 ± 0.7 |
| Predicted metformin CLr,sec (ml/min) (assuming 100% of OCT2 is expressed in the plasma membrane) | 46.2 | 50.4 |
| Predicted metformin CLr,sec (ml/min) (based on % OCT2 expression in the plasma membrane) | 152.98 | 97.7 |
| Predicted metformin CLr,sec (ml/min) based on plasma membrane expression and an average of twofold extrapolation of membrane resting potential based on data by Burt et al. (2016) and Koepsell and Keller (2016) | 305.96 | 195.4 |
| Predicted average CLr,sec (average of 305.96 and 195.4 ml/min) (based on plasma membrane expression and membrane resting potential) | 250.7 | |