Imatinib

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(Redirected from Imatinib mesylate)

Imatinib is a protein kinase inhibitor which binds to a specific amino acid residue within the ATP binding pocket and the activation loop.

In human medicine, this drug has shown efficacy against leukemia, although drug resistance is an emerging phenomenon[1].

In dogs, this drug has been used for treatment of gastrointestinal stromal tumors and hemangiosarcoma[2].

Resistance has been shown with mast cell tumors[3] that show rapid tumor regression but with only temporary remission[4].

The usual starting dose of Imatinib is 20 mg/kg per day.

Large trials of low-dose versus high-dose imatinib in humans did not improve overall survival[5].

References

  1. Kim JH et al (2012) Combined treatment of 3-hydroxyflavone and imatinib mesylate increases apoptotic cell death of imatinib mesylate-resistant leukemia cells. Leuk Res 36(9):1157-1164
  2. Dickerson EB et al (2013) Imatinib and Dasatinib Inhibit Hemangiosarcoma and Implicate PDGFR-β and Src in Tumor Growth. Transl Oncol 6(2):158-168
  3. Hadzijusufovic E et al (2012) NI-1: a novel canine mastocytoma model for studying drug resistance and IgER-dependent mast cell activation. Allergy 67(7):858-868
  4. Kobayashi M et al (2012) Canine intestinal mast cell tumor with c-kit exon 8 mutation responsive to imatinib therapy. Vet J 193(1):264-267
  5. de Matteo RP et al (2009) Adjuvant imatinib mesylate after resection of localised, primary gastrointestinal stromal tumour: a randomised, double-blind, placebo-controlled trial. Lancet 373(9669)':1097–1104