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Inhibition kinetic parameters of icotinib and erlotinib against UGT1A1-mediated NCHN-4-O-glucuronidation in both recombinant human UGT1A1 and HLMs.
| Enzyme source | Icotinib |
Erlotinib |
||||
|---|---|---|---|---|---|---|
| IC50 (μmol/L) | Ki (μmol/L) | Inhibition type | IC50 (μmol/L) | Ki (μmol/L) | Inhibition type | |
| UGT1A1 | 8.76 ± 0.78 | 10.04 | Noncompetitive | 0.69 ± 0.02 | 1.72 | Noncompetitive |
| HLM | 5.15 ± 0.28 | 8.55 | Noncompetitive | 0.68 ± 0.01 | 1.23 | Noncompetitive |
