CYP Isozyme

IC50 for Desvenlafaxine

IC50 for CYP-Specific Inhibitor

CYP1A2

> 100 µM

0.02 µM α-Naphthoflavone

CYP2C8

> 100 µM

10 µM Quercitin

CYP2C9

> 100 µM

1 µM Sulfaphenazole

CYP2C19

> 100 µM

20 µM Tranylcypromine

CYP2D6: Bufuralol cocktaila

50 µM

0.2 µM Quinidine

CYP2D6: Bufuralolb

70 µM

ND

CYP2D6: Bufuralol plus desvenlafaxineb

50 µM

ND

CYP2D6: Dextromethorphanb

80 µM

ND

CYP2D6: Dextromethorphan plus desvenlafaxineb

90 µM

ND

CYP3A4

> 100 µM

0.08 µM Ketoconazole


aProbe utilized as component of a cocktail.
bIn a separate set of experiments, bufuralol and dextromethorphan (5 ĶM) were analyzed separately with the internal standard 4'-hydroxydiclofenac (0.53 ĶM). These substrates were incubated separately so they would not inhibit each otherís metabolism, did not include control incubations containing a known CYP2D6 inhibitor, and the incubations were performed twice; desvenlafaxine 30 ĶM was added to the second set of incubations.
Abbreviations: CYP, cytochrome P450; IC50, half-maximal inhibitory concentration; ND, not determined.
Table 3: Approximate IC50 Values for Desvenlafaxine and Known Inhibitors of Specific CYP Enzymes.
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