This drug is indicated for use against Philadelphia chromosome-positive CML, and is a first line drug in both children and adults.
Imatinib works by inhibiting BCR-abl, which is gene encoding a tyrosine kinase enzyme responsible for phosphorylation of proteins in cancer cells. This enzyme is necessary for cancer growth, and inhibition leads to cancer cell apoptosis.
One of the most common forms of CML arises from the Philadelphia Chromosome, which is a 9;22 translocation. A fusion gene is created as a result of this translocation, elongating chromosome 9 and pairing the ABl gene with the BCR gene from chromosome 22.
Imatinib, or Gleevec, has been used to treat gastrointestinal stromal tumors (GISTs).
This medication works to inhibit tyrosine-protein kinase Kit, or proto-oncogene C-kit. This protein is involved in signaling to play a role in cell survival, proliferation and differentiation, leading to cancerous growth in the GI system.
Though there are various symptoms which arise from Imatinib's use, one of the most severe is fluid retention. This can manifest as edema, but more severely congestive cardiac failure from large doses. Minor side effects include nausea, headache, pancytopenia and growth-delay in children.
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