Table 1.
Cytochrome P450 (CYP450) enzymes involved in the metabolism of EGFR-TKIs approved for the treatment of NSCLC
| Metabolized by CYP | May inhibit | May induce | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 3A4 | 3A5 | 2D6 | 1A1 | 1A2 | 1B1 | 2C8 | 2C9 | 2C19 | 2E1 | |||
| Erlotinib | +++ | +++ | + | + | ++ | + | + | + | – | – | CYP3A4 (m) CYP2C8 (m) CYP1A1 (s) |
CYP1A1 CYP1A2 |
| Gefitinib | +++ | ++ | +++ | ++ | + | – | – | – | – | – | CYP2C19 (w) CYP2D6 (w) | – |
| Afatinib | – | – | – | – | – | – | – | – | – | – | – | – |
| Osimertinib | +++ | +++ | – | – | – | – | – | – | – | – | – | CYP3A (w) |
| Icotinib | +++ | ++ | – | – | +++ | – | – | – | – | +++ | NR | CYP1A2 |
Notes: +++, major metabolic route; ++, other significant metabolic route; +, minor metabolic route; –, no interaction.
Abbreviations: w, weak; m, moderate; s, strong; NR, not reported; EGFR-TKI, epidermal growth factor receptor-tyrosine kinase inhibitor.