TABLE 2

CLint, u, UGT of seven drugs in human kidney, liver, and intestinal microsomes in the presence and absence of bovine serum albumin

Data represent the mean (±S.D.) of n = 3 for human kidney and liver microsomes or n = 1 for human intestinal microsomes. Experiments were performed in duplicate.

Drugfu, incCLint, u, UGT
HLMHKMHIM
− BSAa+ BSAb− BSA+ BSA− BSA+ BSA− BSA+ BSA
μl · min1 · mg protein1
Diclofenac0.98 (0.99, 0.98)0.02761 (105)1190 (195)177 (57)543 (90)74.9325
Ezetimibe0.30 (0.18, 0.18)0.052930 (456)5180 (562)295 (61)495 (105)4181160
Gemfibrozil0.90 (0.90, 0.82)0.01259 (27)1840 (312)265 (6)1910 (488)23.940.0
Mycophenolic acid0.83 (0.91, 0.71)0.1878.2 (4.6)233 (44)293 (58)1370 (187)11.857.8
Naloxone1.00 (1.00, 1.00)0.9610.0 (1.2)55.6 (4.1)10.9 (0.2)52.7 (6.4)0.50214.2
Propofol0.69 (0.69, 0.69)0.2567.8 (4.4)201 (11.4)91.5 (31.9)1023 (130)62.6103
Telmisartan0.65 (0.48, 0.48)0.0776.9 (4.2)395 (57)9.72 (1.58)34.3 (17.3)21.391.4
  • a fu, inc at the protein concentration used for depletion assays in HLM (HKM, HIM) (Supplemental Table 1).

  • b One percent BSA used for diclofenac, gemfibrozil, mycophenolic acid, and telmisartan, and 2% BSA used for ezetimibe, naloxone, and propofol.