TABLE 3

Effects of P450 inhibitors on the metabolism of KRO-105714 in HLMs

InhibitorConcentrationRelative Percentage of Controla
M1M2M3M4
μM%
Control0100100100100
α-Naphthoflavone (CYP1A2)197105122115
5939991113
Tranylcypromine (CYP2A6)190878597
585898379
Quercetin (CYP2C8)59511267132
208811775118
Fluconazole (CYP2C9)5941088476
10991088067
Ticlopidine (CYP2C19)2909897153
10879682131
Quinidine (CYP2D6)1084956276
5073755188
Diethyldithiocarbamate (CYP2E1)20919866110
1009710397105
Ketoconazole (CYP3A4)243484918
1045250.3
  • a Data represent the means of duplicate determinations.