Bidirectional flux studies using MDCK cell monolayers that overexpress human P-gp

Inhibition with 2.5 μM LSN335984. Average values are from duplicate test runs where variability is <22%.

CompoundInhibitorA-B PappB-A Papp%CellaERbNERbCalcein-AM Inhibitionc
Abemaciclib1249684.15.130, 64
Palbociclib6072046128.61, 3
  • A-B, apical to basal; B-A, basal to apical; ER, efflux ratio; NER, net efflux ratio.

  • a Estimated buffer/cell distribution coefficient defined as the fraction of mass that was added to the donor and recovered in the methanol rinse.

  • b ER is B-A Papp/A-B Papp. NER is ER without inhibitor/ER with inhibitor.

  • c Inhibition of Calcein-AM uptake into MDCK–P-gp cells at 5 and 25 μM relative to inhibition using 5 μM LSN335984.