Application of static modeling in the prediction of in vivo drug-drug interactions between rivaroxaban and anti-arrhythmic agents based on in vitro inhibition studies

Data Supplement

Files in this Data Supplement:

• Supplemental Data -

  Supplemental Methods

  Supplemental Figure 1 - Time-dependent (A) A→B and (B) B→A transport of rivaroxaban (10 mu-M)

  Supplemental Figure 2 - Concentration dependent A→B and B→A transport of rivaroxaban (10 to 100 mu-M)

  Supplemental Table 1 - MRM transition and compound-dependent MS parameters of various analytes

  Supplemental Table 2 - Drug-dependent parameters for determination of relevant in vivo

  Results

  Supplemental Figure 3 - (A) Competitive inhibition of CYP2J2 using 5 mu-M amiodarone and 5 mu-M NDEA; (B) Mechanism based inactivation of CYP2J2 by 5 mu-M amiodarone and 5-mu-M NDEA and (C) Mechanism based inactivation of CYP2J2 by 50 mu-M amiodarone and 3 mu-M dronedarone (positive control)

  Supplemental Table 3 - Inactivation efficiency of dronedarone and NDBD against CYP3A4 and CYP2J2 in the presence of different probe substrates

  References