TABLE 2

P450 inhibition of PRN and IPRN in RLM and HLM incubations

The highest concentrations of PRN and IPRN tested in RLM and HLM incubations were 100 µM and 50 µM, respectively. The column headings show human P450 isozymes, and the same substrates were used for RLM studies. n = 3.

ChemicalIC50
CYP1A2CYP2C9CYP2C19CYP2D6CYP3A4
μM
PRN in RLMs10.4 ± 1.41>100>100>100>100
IPRN in RLMs7.1 ± 0.6>100>100>100>100
PRN in HLMs0.26 ± 0.01>50>503.60 ± 0.31>50
IPRN in HLMs0.22 ± 0.03>50>508.49 ± 1.45>50