Representative Lineweaver-Burk plots (A,C) and Dixon plots (B,D) of the effects of erlotinib on SN-38 glucuronide formation in pooled human liver microsomes (A,B) and recombinant UGT1A1 (C,D). Reactions were performed in the presence of SN-38 (2, 5, 7.5, and 10 μM) and various concentrations of erlotinib (0, 0.1, 0.5, 1, and 2 μM) in pooled human liver microsomes (0.5 mg/ml) or recombinant UGT1A1 (0.25 mg/ml), 50 μg/mg protein alamethicin, 5 mM UDPGA, and 10 mM MgCl2 in a 25 mM Tri-HCl buffer (pH 7.4) in a final volume of 200 μl at 37°C for 30 min. All data points shown represent the mean of duplicate measurements.