Enzyme kinetics of ticagrelor metabolite formation in recombinant CYP3A4 and CYP3A5 enzymes

ParameterFormation of AR-C124910XXFormation of AR-C133913XX
CYP3A4CYP3A5CYP3A4CYP3A5
Vmax (pmol/min/pmol)2.17 ± 0.310.38 ± 0.032.22 ± 0.420.38b
Km (μM)11.0 ± 2.55.36 ± 1.2741.3 ± 12.5127b
na1.9
  • Hill factor; others were fitted using the Michaelis-Menten equation.

  • The estimated Km value is above the highest concentration tested (50 μM).