- feeling sick (nausea), diarrhea, headaches, leg aches/cramps, fluid retention, visual disturbances, itchy rash, lowered resistance to infection, bruising or bleeding, loss of appetite, weight gain, reduced number of blood cells (neutropenia, thrombocytopenia, anemia), and edema.
- Severe congestive cardiac failure is an uncommon but recognized side effect of imatinib and mice treated with large doses of imatinib show toxic damage to their myocardium.
- If imatinib is used in prepubescent children, it can delay normal growth, although a proportion will experience catch-up growth during puberty.
Imatinib is rapidly absorbed when given by mouth, and is highly bioavailable and 98% of an oral dose reaches the bloodstream. Metabolism of imatinib occurs in the liverand is mediated by several isozymes of the cytochrome P450 system, including CYP3A4 and to a lesser extent, CYP1A2, CYP2D6, CYP2C9, and CYP2C19. The main metabolite, N-demethylated piperazine derivative, is also active. The major route of elimination is in the bile , feces and only a small portion of the drug is excreted in the urine. Most of imatinib is eliminated as metabolites. only 25% is eliminated unchanged. The half-lives of imatinib and its main metabolite are 18 and 40 hours, respectively. It blocks the activity of Abelson cytoplasmic tyrosine kinase (ABL), c-Kit and the platelet-derived growth factor receptor (PDGFR). As an inhibitor of PDGFR, imatinib mesylate appears to have utility in the treatment of a variety of dermatological diseases. Imatinib has been reported to be an effective treatment for FIP1L1-PDGFR alpha mast cell disease, hypereosinophilic syndrome, and dermatofibrosarcoma protuberans