HIV Inhibitor | Ki | αKi | Inhibition Mechanism | Predicted Inhibition at Csse |
---|---|---|---|---|
μM | % | |||
Atazanavirb | 1.9 | 16.4 (α = 8.6) | Linear mixed | 28.7 |
Indinavirc | 47.9 | 1317 (α = 27.5) | Linear mixedd | 2.5 |
↵ a Human cDNA-expressed UGT1A1 in lymphoblast cells.
↵ b UGT1A1: apparent Km = 4 μM and Vmax = 80 pmol/min mg protein in this set of experiments.
↵ c UGT1A1: apparent Km = 2.8 μM and Vmax = 62 pmol/min mg protein in this set of experiments.
↵ d A noncompetitive mechanism with a Ki = 100 μM was reported (Food and Drug Administration summary basis of approval, indinavir).
↵ e For atazanavir, Css = 1.73 μM (400 mg q.i.d.); for indinavir, Css = 3.84 μM (Crixivan package insert, 800 mg t.i.d.); [bilirubin] = 6.84 μM.