Table 3.
Intrinsic Clearance (CLINT) in Human Microsomes and Predicted Hepatic Clearance (CLHEP) of Analogous Triazole and Amide-Containing CFTR Modulators.
| 1,2,3-triazole | amide | ||||
|---|---|---|---|---|---|
| cmpd | CLINT[a] (mL min−1 kg −1) | CLHEP[b] (mL min−1 kg −1) | cmpd | CLINT[a] (mL min−1 kg −1) | CLHEP[b] (mL min−1 kg −1) |
| 11 | 11.8 | 7.55 | 23 | 2.49 | 2.23 |
| 20 | 23.2 | 11.0 | 26 | 36.1 | 13.3 |
| 56 | 16.3 | 9.19 | 36 | 12.5 | 7.84 |
| 58 | 19.3 | 10.1 | 37 | 9.35 | 6.47 |
| 60 | 56.2 | 15.3 | VX-770 | 45.6 | 14.4 |
Intrinsic clearance in human hepatic microsomes.
Predicted hepatic clearance, human.