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Table 2 The inhibition and induction parameters of CYP3A4 and CYP1A2 perpetrators

From: Prediction of drug–drug interactions between roflumilast and CYP3A4/1A2 perpetrators using a physiologically-based pharmacokinetic (PBPK) approach

Perpetrators

CYP3A4 Ki (μM)

CYP1A2 Ki (μM)

ECmax

EC50 (μM)

Ketoconazole (inhibitor, KET) [27]

0.0054

32

  

Itraconazole (inhibitor, ITR) [28]

0.0013

 

-

-

Hydroxy-itraconazole [28]a

0.0023

 

-

-

Fluconazole (inhibitor, FLU) [29]

16.6

 

-

-

Fluvoxamine (inhibitor, FLUV)b

0.52

0.011

-

-

Enoxacin (inhibitor, ENO) [30]

-

110

  

Cimetidine (inhibitor, CIM) [31, 32]

106

140.7

  

Rifampicin (inducer, RIF) [28]

-

-

9.0

0.34

Efavirenz (inducer, EFA)b

-

-

5.2

0.07

  1. ametabolite of itraconazole
  2. bbuilt in the PK-Sim