Compound | Rslope (%CV) s−1 × 10−6 | Flux Dialysis fua | Reported fu (Reference) |
---|---|---|---|
Imipramine | 0.13 (Berry et al., 2011) | ||
38.9 (23%) | 0.14 | ||
Quinidine | 31.1 (8%)b | 0.11 | 0.22 (Fremstad et al., 1979) |
Sertraline | 9.72 (8%)b | 0.035 | 0.016 (Ronfeld et al., 1997) |
Glecaprevir | 6.67 (21%) | 0.024 | 0.025 (AbbVie data on file) |
Indomethacin | 2.61 (13%) | 0.0094 | 0.010 (Indomethacin, 2016) |
Nelfinavir | 0.778 (7%)b | 0.0028 | 0.0042 (Motoya et al., 2006) |
Itraconazole | 0.583 (5%) | 0.0021 | 0.0021 (Riccardi et al., 2015) |
Glyburide | 0.317 (6%) | 0.0011 | 0.0010 (Wan and Rehngren, 2006) |
Lapatinib | 0.211 (10%) | 0.00076 | <0.011 (U.S. FDA, 2007) |
UCN-01 | 0.0247 (1%) | 0.000089 | 0.000073c (Fuse et al., 1998) |
Pibrentasvir | 0.0172 (33%) | 0.000062 | <0.0001 (AbbVie data on file) |
Amiodarone | 0.0158 (8%) | 0.000057 | 0.00014 (Riccardi et al., 2015) |
Bedaquiline | 0.00806 (15%) | 0.000029 | <0.0001 (U.S. FDA, 2012) |
Venetoclax | 0.00333 (32%) | 0.000012 | 0.000013 (AbbVie data on file) |
%CV, interassay %CV calculated from experiments conducted on separated days (n = 2–5 experiments); %CV values for flux dialysis fu are identical to Rslope %CV and therefore are not reported separately.
↵a Calculated as Rslope × 3590 s.
↵b Intra-assay %CV calculated from a single experiment run in triplicate.
↵c fu value calculated from published Bmax and KD values (i.e., fu = KD/(KD + Bmax) = 0.0012/(0.0012 + 16.4) = 0.000073).