Table 1.

Comparison of Potency and Response to BCR-ABL1 TKIs

Drug	BCR-ABL1 Cellular IC50 (nM)	Plasma Half-Life (h)	Frontline Treatment at 1 Year			Frontline Treatment at 5 Years
			Rate of CCR (%)	Rate of MMR (%)	Rate of MR4.5 (%)	Rate of MR4.5 (%)	PFS (%)
Imatinib 400 mg	100–500	18	55–66	22–38	1–5	30–35	86–91
High-dose Imatinib			65	45–55	9	58a	89
Dasatinib	0.8–1.8	3–5	77	46	5	42	85
Nilotinib	10–25	17	80	44	11	54	96
Bosutinib	42	32–39	77	47	8.1	NA	NA
Ponatinib	0.5	22	100b	80b	60b	NA	NA
Asciminib	0.25	8	48b	NA	NA	NA	NA

NA, data not yet available.

Data summarized from the following references: IC₅₀ values (Rossari et al., 2018); half-life (Abbas et al., 2012; Cortes et al., 2012; Hazarika et al., 2008; Peng et al., 2004; Reckel et al., 2017); dasatinib versus imatinib (Cortes et al., 2016; Kantarjian et al., 2010); nilotinib versus imatinib (Hochhaus et al., 2016; Saglio et al., 2010); bosutinib versus imatinib (Cortes et al., 2018a); ponatinib versus imatinib (Lipton et al., 2014, 2016); high-dose versus standard-dose imatinib (Gafter-Gvili et al., 2011; Hehlmann et al., 2017).

^aMR^4.5 rate for standard dose imatinib in CML IV study was 49%.

^bOnly ten patients on ponatinib in the EPIC trial reached 1 year.