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. Author manuscript; available in PMC: 2020 Mar 7.
Published in final edited form as: Chemistry. 2019 Feb 11;25(14):3662–3674. doi: 10.1002/chem.201805919

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
[a]

Intrinsic clearance in human hepatic microsomes.

[b]

Predicted hepatic clearance, human.