TABLE 3

Comparison of risks generating overestimation or underestimation of Apparent permeability coefficient (Papp) and P-glycoproteain properties of dabigatran etexilate among four experimental settings

SubstrateDetection±BNPPAtoB (Dabigatran Etexilate Conc.)BtoA (Dabigatran Etexilate Conc.)Efflux Ratio
[14C]Dabigatran etexilateLSCDonorLarge overestimationDonorCorrectIncorrect
ReceiverLarge overestimationReceiverSmall overestimation
[14C]Dabigatran etexilateLSC+DonorSmall overestimationDonorCorrectIncorrect
ReceiverModerate overestimationReceiverCorrect
Dabigatran etexilateLC-MS/MSDonorLarge reductionDonorCorrectIncorrect
ReceiverCorrectReceiverCorrect
Dabigatran etexilateLC-MS/MS+DonorCorrectDonorCorrectCorrect
ReceiverCorrectReceiverCorrect
  • AtoB, apical to basa; BNPP, bis(p-nitrophenyl) phosphate; BtoA, basal to apical; CsA, cyclosporin A; LC-MS/MS, liquid chromatography-tandem mass spectrometry; LSC, liquid scintillation counter.