Table 3. Comparison of FDA Appproved Abl Kinase Inhibitors.

A comparison of the pharmacokinetic and pharmacodynamic properties, and the edema-related side effects, of the Abl kinase inhibitors that are currently in clinical usage^{60, 84}

Drug	Imatinib	Dasatinib	Nilotinib	Ponatinib	Bosutinib
Off Target Effects	c-KIT, PDGFR, DDR1, NQO2	c-KIT, PDGFR, DDR1/2, SRC, YES, FYN, LYN, HCK, LCK, FGR, BLK, FRK, CSK, BTK, TEC, BMX, TXK, ACK, BRAF, EGFR, EPHA, MAPK, RAF, SLK, ZAK	c-KIT, PDGFR, DDR1, NQO2 More specific to Abl kinases	c-KIT, PDGFR, FLT3, FGFR, RET, VEGFR, SRC Inhibits mutant BCR-Abl forms including T315I.	ALK, CSK, FGR,LYN, PKA, CK1, CK2, SRC, RET,SYK
T1/2 (hrs)	18	3–5	15–17	24	22.5
F (%)	98	<34	30	65	unknown
Vd (L/kg)	2–6	36	2	17.5	87
Metabolism	CYP3A4 CYP3A5 CYP2C8	CYP3A4	CYP3A4 CYP2C8	CYP3A4 CYP3A5 CYP2C8 CYP2D6	CYP3A4
Edema (%)	53	50	11	13–22	14

F – Bioavailability, Vd – Volume of Distribution.