TABLE 1

IC50 values of HIV PIs against PMAT and OCT1–3

Concentration-dependent inhibition experiments were conducted on PMAT and OCT1–3 with IDT307 or ASP+ assays. IC50 values were determined by nonlinear regression fit as described in Materials and Methods. Shown are the mean ± S.D. values from three independent kinetic experiments.

HIV PIIC50 (µM)
PMATOCT1OCT2OCT3
IndinavirNI33.4 ± 6.8aNINI
Amprenavir51.5 ± 8.8a40.4 ± 7.3aNINI
Nelfinavir44.6 ± 8.0a60.5 ± 10.9aNINI
Atazanavir49.5 ± 7.5aNININI
Tipranavir8.9 ± 2.838.0 ± 5.8aNINI
Lopinavir1.4 ± 0.2174 ± 40.1aNINI
Ritonavir6.0 ± 0.511.2 ± 3.578.9 ± 19.7a59.8 ± 9.3a
Saquinavir7.0 ± 1.044.8 ± 12.0aNINI
  • NI, no significant concentration-dependent inhibition.

  • a Partial inhibition at the highest concentration tested (50 µM) due to limited drug solubility.