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Newly Diagnosed Patients
Imatinib-resistant/intolerant
Mechanism of Action
Dosing TASIGNA

MECHANISM OF ACTION

Bcr-Abl is the key cause and driver of Ph+ CML

Ph+ CML is a disease of Bcr-Abl. Bcr-Abl is the single, definitive cause of Ph+ CML and remains the key driver of the disease throughout the chronic phase,1,2 giving no rationale for targeting additional kinases in the treatment of Ph+ CML-CP. Imatinib confirmed Bcr-Abl as an effective target in Ph+ CML, but because a significant subset of patients developed resistance or intolerance to imatinib, Novartis Oncology scientists continued the search for a Ph+ CML therapy that would more effectively target Bcr-Abl.3

Bcr-Abl mechanism of disease video
Bcr-Abl mechanism of disease video
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INTERACTIVE GAME
TASIGNA Interactive Game
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The ENESTnd study showed that newly-diagnosed TASIGNA patients achieve faster and deeper reductions in Bcr-Abl and have lower rates of progression than imatinib patients.4

TASIGNA was designed to be a more potent and selective inhibitor of Bcr-Abl than imatinib3

TASIGNA and imatinib binding structures
TASIGNA and imatinib binding structures
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  • TASIGNA is the most selective Bcr-Abl inhibitor
  • Better topological fit for the kinase-binding domain
    • More able to bind to mutant forms of Bcr-Abl


References:
1. Shah NP, Nicoll JM, Nagar B, et al. Multiple Bcr-Abl kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell. 2002;2(2):117-125.
2. Hochhaus A, Kreil S, Corbin AS, et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia. 2002;16(11):2190-2196.
3. Weisberg E, Manley PW, Cowan-Jacob SW, Hochhaus A, Griffin JD. Second generation inhibitors of Bcr-Abl for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer. 2007;7(5):345-356.
4. TASIGNA® (nilotinib) Summary of Product Characteristics. Basel, Switzerland: Novartis Pharma AG; December 2010.

TASIGNA delivered the deepest measurable reductions in Bcr-Abl levels in more patients with newly diagnosed Ph+ CML than imatinib.4

TASIGNA demonstrated superior efficacy head-to-head vs. imatinib in patients with newly diagnosed Ph+ CML.4

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