TABLE 1

Ki (μM)a values for competitive inhibition of P450 isoforms by deleobuvir, CD 6168, and deleobuvir-AG

P450 IsoformDeleobuvirCD 6168Deleobuvir-AG
TotalFreebTotalFreeTotalFree
CYP1A2NANANANA12.56.13
CYP2B617.511.3NANA20.49.99
CYP2C80.130.0870.270.210.0220.0108
CYP2C94.73.01813.514.47.06
CYP2C19NANANANA2612.7
CYP2D6NANANANA5024.5
CYP3A47.44.42317125.88
  • NA, no inhibition up to the highest concentration tested (50 or 75 μM)

  • a Calculated as IC50 × 0.5, assuming competitive inhibition.

  • b Adjusted for protein binding in HLM.