Table 2.
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.