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. Author manuscript; available in PMC: 2013 Mar 1.
Published in final edited form as: J Pharmacol Toxicol Methods. 2012 Feb 26;65(2):64–74. doi: 10.1016/j.vascn.2012.02.002

Table 2.

Data for correlations of IC50 values for various drugs determined using Fl-t-pgp with in vivo effects on digoxin disposition in humans

Digoxin in vivo [inhibitor] in vivo Fl-t-pgp
Drug AUCI/AUC Cmax,ss,I/Cmax,ss [I]a [I2]b IC50,Flc [I]/IC50,Fl [I2]/IC50,Fl
Diltiazem 1.44 1.38 0.7 532 24.2 0.02893 21.98
Quinidine 1.76 1.75 3.54 3397 2.5 1.416 1359
Telmisartan 1.22 1.58 1.11 933 0.12 9.250 7775
Troglitazone 1.04 1.05 3.62 3264 5.2 0.6961 627.7
Verapamil 1.51 1.44 1.2 652 11.9 0.1008 54.79
Carvedilol 1.56 1.38 0.13 61.5 3.8 0.03421 16.18
Felodipine 1.18 1.34 0.03 104 16.5 0.001818 6.303
Mibefradil 1.31 1.41 2.42 1211 7.1 0.3408 179.0
Nicardipine 1.06 1.06 0.18 248 0.93 0.194 266.7
Ranolazine 1.6 1.46 8.4 9356 64.1 0.1310 146.0
Amiodarone 1.68 1.84 2.2 4693 2.6 0.8461 1805
Isradipine 1.11 1.26 0.02 161.5 6.6 0.003030 24.47
Sertraline 1.1 1.05 0.39 2612 29 0.01345 90.07
Captopril 1.39 1.59 0.23 230 429 0.0005361 0.5361
Nifedipine 1.23 1.06 0.23 115.5 2.6 0.08846 44.42
Nitrendipine 1.15 1.57 0.03 222.0 5.8 0.005172 38.28
a

Peak plasma concentration of drug (“inhibitor”) at steady state, in µM; data taken from Fenner et al. (Fenner et al., 2009).

b

Estimated gastrointestinal concentration of drug (“inhibitor”) after oral dose, in µM; data taken from Fenner et al. (Fenner et al., 2009).

c

Half-maximal concentration for inhibition of transport in Fl-t-pgp by drug (“inhibitor”), in µM.