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. 2019 Oct 25;9:1132. doi: 10.3389/fonc.2019.01132

Table 2.

Indications of currently available TKI in advanced phase of chronic myeloid leukemia.

TKI Relative potency against BCR-ABL1 Other targets Indications in AP Indications in BP
Imatinib 1 (reference) PDGFR > c-KIT AP-CML or BP-CML
Nilotinib ≈25 PDGFR AP-CML with resistance of intolerance to prior therapy including imatinib Not indicated
Dasatinib ≈325 Src > BTK > PDGFR > c-KIT AP-CML or BP-CML with resistance of intolerance to prior therapy including imatinib
Bosutinib ≈15 BTK > Src AP-CML or BP-CML previously treated with one or more TKI (s) and for whom imatinib, nilotinib and dasatinib are not considered appropriate treatment options (EMA)
AP-CML or BP-CML with resistance or intolerance to prior therapy (FDA)
Ponatinib ≈900 PDGFR > VEGFR2 > Src > c-KIT AP-CML or BP-CML who are resistant to dasatinib or nilotinib; who are intolerant to dasatinib or nilotinib and for whom subsequent treatment with imatinib is not clinically appropriate; or who have the T315I mutation (EMA)
AP-CML or BP-CML resistant or intolerant to prior TKI therapy (FDA)

AP, accelerated phase; BP, blast phase; PDGFR, Platelet-derived Growth Factor Receptor; BTK, Bruton's Tyrosine Kinase; TKI, Tyrosine Kinase Inhibitors; EMA, European Medicine Agency; FDA, Food and Drug Administration.