Comparative Pharmacology of Tyrosine Kinase Inhibitors for the Treatment of Chronic Myeloid Leukemia : Table 4

Table 4: Metabolism and metabolite activity of BCR/ABL inhibitors.

	Enzymes	Metabolites	Metabolite activity
Bosutinib	CYP3A4	Oxide chlorinated derivative (M2) Demethylated derivative (M5)	Very reduced Very reduced
Dasatinib	CYP3A4	Oxide derivatives Derivatives conjugated with glucoronic acid	Inactive
Imatinib	CYP3A4, CYP1A2, CYP2D6, CYP2C9, CYP2C19	N-desmetilimatinib	Similar to imatinib
Nilotinib	CYP3A4, CYP2C8, UGT1A1	Oxide derivatives Derivatives conjugated with glucoronic acid	Probably inactive
Ponatinib	Amidases, esterases CYP3A4, CYP2C8, CYP2D6, CYP3A5	N-demethylated	Inferior