Which medications in the drug class Tyrosine Kinase Inhibitors are used in the treatment of Chronic Myelogenous Leukemia (CML)?

Updated: May 23, 2021
  • Author: Emmanuel C Besa, MD; Chief Editor: Sara J Grethlein, MD, FACP  more...
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Answer

Tyrosine Kinase Inhibitors

Tyrosine kinase inhibitors elicit strong inhibition of tyrosine kinase activity of the BCR/ABL abnormality in all phases of CML.

Imatinib mesylate (Gleevec)

Imatinib is specifically designed to inhibit the tyrosine kinase activity of BCR-ABL kinase in Ph1-positive leukemic CML cell lines. It is indicated for treatment of Ph+ CML in chronic phase (newly diagnosed) in adults and children and treatment of Ph+ CML in blast crisis, accelerated phase, or chronic phase after failure of interferon-alfa therapy.

Dasatinib (Sprycel)

Dasatinib is a multiple tyrosine kinase inhibitor. It inhibits growth of cell lines overexpressing BCR/ABL. It has been able to overcome imatinib resistance resulting from BCR/ABL kinase domain mutations.

Dasatinib is indicated for newly diagnosed adults with Philadelphia chromosome-positive (Ph+) CML in chronic phase, adults with chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib, adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy, and pediatric patients with Ph+ CML in chronic phase.

Nilotinib (Tasigna)

Nilotinib is a selective tyrosine kinase inhibitor that targets BCR-ABL kinase, c-KIT and platelet derived growth factor receptor (PDGFR). Nilotinib inhibits BCR-ABL mediated proliferation of leukemic cell lines by binding to the ATP-binding site of BCR-ABL and inhibiting tyrosine kinase activity. Nilotinib has activity in imatinib-resistant BCR-ABL kinase mutations. It is indicated in adults for the treatment of newly diagnosed Ph+ CML and chronic or accelerated phase Ph+ CML resistant to or intolerant to prior therapy that included imatinib. Also indicated in pediatric patients (≥1 year) for the treatment of newly diagnosed Ph+ CML and chronic phase Ph+ CML resistant or intolerant to prior tyrosine-kinase inhibitor (TKI) therapy.

Bosutinib (Bosulif)

Bosutinib is a tyrosine kinase inhibitor. It inhibits the Bcr-Abl kinase that promotes CML, and it also inhibits SRc-family kinases, including Src, Lyn, and Hck. It inhibits 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines, but does not inhibit T315I and V299L mutant cells. This kinase inhibitor indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy. It also indicated for newly-diagnosed chronic phase Ph+ CML.

Ponatinib (Iclusig)

Ponatinib is a kinase inhibitor indicated for patients with CML or Ph+ ALL that is resistant or intolerant to prior tyrosine kinase inhibitor therapy, including those with the T315I mutation. Because of its high risk for thromboembolic events, it is indicated for patients with T315I-positive, Ph+ ALL for whom no other TKI therapy is indicated.


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