Dual EGFR and ABL Tyrosine Kinase Inhibitor Treatment in a Patient with Concomitant EGFR-Mutated Lung Adenocarcinoma and BCR-ABL1-Positive CML

Table 1

Contribution ratio of CYP3A4 to clearance of EGFR-TKIs after oral absorption (CR_CYP3A4).

	Calculated CRCYP3A4	Standard inhibitor	AUC fold change by standard inhibitor	Reference
Gefitinib	0.46	Itraconazole	1.78	[13]
Erlotinib	0.40	Ketoconazole	1.68	[14]
Afatinib	0
Osimertinib	0.20	Itraconazole	1.24	[15]

IR_CYP3A4 values for itraconazole and ketoconazole are 0.95 and 1.00, respectively (Ref. [5]). Substrate for the P-glycoprotein (P-gp). Metabolism by cytochrome P-450 is of negligible (Ref. [16]).