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Metabolism of tacrolimus in the presence of voriconazole. Tacrolimus (0 to 20 μM) was incubated in the absence (•) or in the presence (▾) of 200 μg of voriconazole/ml, and the amount of tacrolimus metabolized was estimated by HPLC. The figure shows that voriconazole decreases the maximal velocity of tacrolimus metabolism (Vmax, 1.47 to 0.37 nmol/min/mg of protein) and changes the affinity of tacrolimus for the enzyme (Km, 10.64 to 5.43 μM).
