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. 2015 Dec 8;5:17778. doi: 10.1038/srep17778

Table 3. The inhibition kinetic parameters and types of TKIs on UGTs.

enzymesresource Substrate Ki (μM)/inhibition type
Imatinib Lapatinib Vandetanib
UGT1A1 4-MU 19.1 ± 2.8/competitive 0.5 ± 0.1/competitive
UGT1A1 SN-38 0.6 ± 0.1/competitive
UGT1A4 TFP 36.4 ± 5.0/mixed
UGT1A7 4-MU 4.5 ± 0.5/noncompetitive
UGT1A9 4-MU 9.0 ± 1.2/mixed
UGT2B17 4-MU 0.4 ± 0.1/competitive
HLMs SN-38 1.6 ± 0.2/noncompetitive