Table 1.
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).
MR4.5 rate for standard dose imatinib in CML IV study was 49%.
Only ten patients on ponatinib in the EPIC trial reached 1 year.