TABLE 2

Correlation analysis of fingolimod metabolism rates with marker enzyme activities in a panel of HLM from individual donors

EnzymeMarker ReactionCorrelation (R value)
CYP1A2Phenacetin O-deethylation0.08
CYP2A6Coumarin 7-hydroxylation0.2
CYP2B6(S)-Mephenytoin N-demethylation0.25
CYP2C8Paclitaxel 6α-hydroxylation0.18
CYP2C9Diclofenac 4′-hydroxylation0.4
CYP2C19(S)-Mephenytoin 4′-hydroxylation0.03
CYP2D6Bufuralol 1′-hydroxylation0.39
CYP2E1Chlorzoxazone 6-hydroxylation0.32
CYP3A4/5Testosterone 6β-hydroxylation0.32
CYP4ALauric acid 12-hydroxylation0.32
FMOMethyl p-tolyl sulfide oxidation0.4