Imatinib

Pharmacogenomic Information in the Context of the FDA-Approved Drug Label*

The decision of whether to treat patients with imatinib is based on the presence of genetic biomarkers, including BCR-ABL (the Philadelphia chromosome), KIT, and PDGFR gene rearrangements.

Excerpt from the imatinib drug label:

"Gleevec is a kinase inhibitor indicated for the treatment of:

• Newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase.
  . . .
• Adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements (1.5)
  Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown (1.6)
  . . .
• Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST). (1.9)
• Adjuvant treatment of adult patients following resection of Kit (CD117) positive GIST (1.10)"

Imatinib is an inhibitor of the BCR-ABL tyrosine kinase that is created by the Philadelphia chromosome rearrangement in chronic myeloid leukemia. Imatinib also inhibits the kinases encoded by the PDGFRB and KIT genes. The KIT:D816V mutation, found in many patients with aggressive systemic mastocytosis, is a gain-of-function mutation that is resistant to treatment with imatinib.

(For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Imatinib drug label PDF.)

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