TABLE 2

IC50 determination for inhibition of UGTs by HIV protease inhibitors

HIV Inhibitor
IC50 Valuesa
UGT1A1
UGT1A3
UGT1A4
UGT1A6
UGT1A9
UGT2B7
μM
Atazanavir 2.3 7.9 21 >100 >100 >100
Indinavir 87b 26 >100 >100 >100 >100
Saquinavir 13 5.5 8.0 >100 >100 >100
Lopinavir 8.6 3.9 7.6 >100 >100 >100
Ritonavir 19 6.3 2.0 >100 >100 >100
Nelfinavir
11
60
55
>100
>100
>100

  • ↵ a Human cDNA-expressed UGT1A1 in baculovirus-infected insect cells.

  • ↵ b The value was 87 μM from a determination in cDNA-expressed UGT1A1 in lymphoblast cells as described in Table 3. The IC50 value was 111 μM from the determination in cDNA-expressed UGT1A1 in baculovirus-infected insect cells.