Inhibitor

µM

Enzyme Inhibited

Percent Inhibition of NODV Formationa

Percent Inhibition of Benzyl Hydroxyl Desvenlafaxine Formationa

α-Naphthoflavone

1

CYP1A2

0

0

Coumarin

100

CYP2A6

0

0

Sulfaphenazole

10

CYP2C9

21

0

S(+)-Mephenytoin

100

CYP2C19

0

0

Quinidine

10

CYP2D6

4

0

Diethyldithiocarbamate

100

CYP2E1

15

19

Ketoconazole

50

5

1

CYP3A4

CYP3A4

CYP3A4

76

65

29

58

29

0

Benzylimidazole

1000

All CYPs

87

99

Heat inactivation

1 min at 50°C

FMO

0

0

aValues are expressed as percent inhibition relative to a control reaction using the formula: % inhibition = ([a - b]/a * 100%), where a = peak area of metabolite with no inhibitor present, and b = peak area of metabolite with inhibitor present.
Abbreviations: CYP, cytochrome P450; FMO, flavin-containing monooxygenase.
Table 1: Inhibition of Desvenlafaxine Metabolism by Specific Isozyme Inhibitors in Human Liver Microsomes.
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