The mechanism of action shows inhibition of cells expressing native or mutant BCR::ABL1, including T315I1,4-7
Ponatinib mechanism of action (MOA)
Ponatinib is the only pan-mutational TKI that was purposefully engineered to inhibit BCR::ABL1 with or without mutations1,4-8
- Binds to the ATP binding site of BCR::ABL1
- Inhibits the activity of BCR::ABL1, leading to cell death
- Shows activity against all known single-point mutations, including T315I
According to the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for CML: Ponatinib (ICLUSIG) has no contraindicated BCR::ABL1 mutations.3
ATP= Adenosine triphosphate; CP-CML=chronic phase chronic myeloid leukemia; CP=chronic phase; Ph+ ALL= Philadelphia Chromosome positive acute lymphoblastic leukemia; TKI=tyrosine kinase inhibitor.