Table 2 A summary of metabolism of EGFR TKIs drugs
EGFR TKIs | Generation | Metabolism | Drug-drug interactions | MDRP substrates |
|---|---|---|---|---|
Gefitinib | First | CYP3A4, CYP2D6, CYP3A5 (minor) | â–ª CYP3A4, CYP2D6 inhibitors may increase serum concentration â–ª CYP3A4, CYP2D6 inducers may decrease serum concentration | P-gp and BCRP |
Erlotinib | First | CYP1A2, CYP3A4 | â–ª CYP3A4, CYP2A1 inhibitors may increase serum concentration â–ª CYP3A4, CYP2A1 inducers may decrease serum concentration â–ª Erlotinib reduce serum concentrations of other CYP3A4 substrates | P-gp and BCRP |
Afatinib | First | None | â–ª P-gp inhibitors may increase serum concentration â–ª P-gp inducers may decrease serum concentration | P-gp and BCRP |
Dacomitinib | Second | CYP2D6 | â–ª CYP2D6 inhibitors may increase serum concentration | None |
Osimertinib | Third | CYP3A4 | â–ª CYP3A4 inhibitors may increase serum concentration â–ª CYP3A4 inducers may decrease serum concentration â–ª Osimertinib may increase serum concentrations of other P-gp/BCRP substrates | P-gp and BCRP |
Mobocertinib | Third? | CYP3A4, CYP3A5 | â–ª CYP3A4/5 inhibitors may increase serum concentration â–ª CYP3A4/5 inducers may decrease serum concentration | Unknown |