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. Author manuscript; available in PMC: 2020 Dec 8.
Published in final edited form as: Cancer Cell. 2020 Apr 13;37(4):530–542. doi: 10.1016/j.ccell.2020.03.006

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).

a

MR4.5 rate for standard dose imatinib in CML IV study was 49%.

b

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