TABLE 1

Effect of E-sul on the uptake of telmisartan and E217β G by cryopreserved human hepatocytes in the presence of 0.3% HSA

The substrate concentration used was 0.1 and 1 μM for telmisartan and E217β G. Saturable uptake of telmisartan and E217β G into cryopreserved human hepatocytes was determined after the subtraction of nonsaturable uptake (evaluated as the uptake clearance of the respective compounds in the presence of 40 μM telmisartan and 200 μM E217β G). In parentheses is the percentage of the saturable uptake of telmisartan and E217β G in the absence of inhibitor.


E-sul

HH-OCF

HH-094

HH-MYO
Telmisartan
E217βG
Telmisartan
E217βG
Telmisartan
E217βG
μl/min/106 cells μl/min/106 cells μl/min/106 cells
0 μM 48.5 ± 3.6 5.66 ± 1.1 42.0 ± 1.7 1.85 ± 0.72 16.8 ± 5.3 2.01 ± 0.62
30 μM 63.9 ± 11 1.50 ± 0.75 42.2 ± 0.41 1.03 ± 0.76 18.1 ± 3.7 0.38 ± 0.45

(131%)
(26.6%)
(100%)
(55.8%)
(108%)
(19.0%)