Table 2

Ki values for the inhibition of wild-type and patient HIV-1 proteases by clinically available inhibitors

PIaKi value (nM)bRelative resistancec
Wild-type HIV-1 PRPatient HIV-1 PR
SQV0.04 ± 0.017,500 ± 400190,000
RTV0.015 ± 0.003190 ± 1013,000
IDV0.12 ± 0.02860 ± 407,200
NFV0.07 ± 0.01250 ± 103,600
APV0.18 ± 0.0214 ± 177
LPV0.018 ± 0.00916 ± 2870
ATV0.024 ± 0.00594 ± 53,900
TPV0.14 ± 0.020.049 ± 0.0020.35
DRV0.0053 ± 0.00360.059 ± 0.00711
  • a The protease inhibitors (PIs) were saquinavir (SQV), ritonavir (RTV), indinavir (IDV), nelfinavir (NFV), amprenavir (APV), lopinavir (LPV), atazanavir (ATV), tipranavir (TPV), and darunavir (DRV).

  • b The inhibition constants were determined by spectrophotometric assay at the pH optimum of the protease (PR) (pH 4.7). Values are means ± standard deviations for 3 independent assays.

  • c Relative resistance was calculated as follows: Ki of the patient's HIV-1 PR/Ki of the wild-type HIV-1 PR.