Table 1.

The main TKIs approved for CML patients during the various phases of the disease, their molecular targets and BCR-ABL mutations responsible for drug resistance in CML patients.

Drugs	Molecular target of the drugs	Indications of drug use for CML patients at various phases of the disease	BCR-ABL mutations responsible for drug resistance in patients	Ref
Imatinib	BCR-ABL	First line TKI in CML (all phase)	Y253F/H; E255K; M351T; F359V; T315I; F317L; Q252H/R	(22–261)
		For adult and children with a new diagnosis of CML or not eligible for bone marrow transplant.
Nilotinib	BCR-ABL	For CML-CP and -AP patients resistant or intolerant to other options, such as Imatinib.	T315I	(27–302)
		For newly diagnosed CML-CP patients.
Dasatinib	BCR-ABL/Src	First line TKI for newly diagnosed CML patients.	Less sensitive mutations: Y253H; E255V/K, F359V/CT315I	(28, 31–33)
		For resistance or intolerance to other drugs, including Imatinib, in all CML phases.	Less sensitive mutations: V299L; F317L
Bosutinib	BCR-ABL/Src	After intolerance or resistance to prior therapy.	T315I	(34–373,4)
		For newly diagnosed-CML patients as first line TKI drug
Ponatinib	BCR-ABL, Src, Akt	For all phase CML patients resistant or intolerant to prior TKI therapy.	Compound mutations in CML-AP (T315I/E453K) and CML-BP (T315I/F359C) patients	(38–425)
		In presence of T315I BCR-ABL mutation in all CML phases

¹https://www.ema.europa.eu/en/documents/overview/glivec-epar-summary-public_en.pdf.

²https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022068s000_LBL.pdf.

³https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/20334s007s008lbl.pdf.

⁴https://www.ema.europa.eu/en/documents/overview/bosulif-epar-medicine-overview_en.pdf.

⁵https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/203469s022lbl.pdf.