Imatinib mesylate (STI 571) is one of the fundamental chemotherapeutic agents used in the treatment of the chronic, accelerated and blastic phases of chronic myelocytic leukemia (CML), gastrointestinal stromal tumors and Philadelphia chromosome-positive acute lymphoblastic leukemia. It selectively inhibits receptor tyrosine kinases. Its effects limit the use of this drug. We present a case with...

1. Cohen MH, Williams G, Johnson JR, et al. Approval summary for imatinib mesylate capsules in the treatment of chronic myelogenous leukemia. Clin Cancer Res. 2002;8:935-942. 2. Hoelzer D, Gokbuget N, Ottman OG. Targeted therapies in the treatment of Philadelphia chromosome–positive acute lymphoblastic leukemia. Semin Hematol. 2002;39(suppl 3):32-37. 3. Dager R, Cohen M, Williams G, et al. Appr...

Imatinib mesylate is a small-molecule tyrosine kinase inhibitor (TKi) designed to target c-ABL and BCR-ABL, approved for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. Adverse cutaneous reactions induced by imatinib are frequent, generally moderate, and dose-dependent. The aim of this work was to investigate the possible contribution of interleukin (IL)-33 and IL...

The objective of the current study is to develop a validated, specific and stability-indicating reverse phase liquid chromatographic method for the quantitative determination of genotoxic impurities in the drug substance imatinib mesylate. This report includes a brief review of the toxicology of impurities in imatinib mesylate and the strategies used to set acceptance criteria for genotoxic imp...

Recent cancer molecular therapies are targeting main functional molecules to control applicable process of cancer cells. Attractive targets are established by receptor tyrosine kinases, such as platelet-derived growth factor receptors (PDGFRs) and c-Kit as mostly irregular signaling, which is due to either over expression or mutation that is associated with tumorigenesis and cell proliferation....

A 70-year-old man developed severe periorbital edema secondary to imatinib mesylate (Gleevec; Novartis Pharmaceuticals Corp, East Hanover, NJ). Imatinib mesylate is a tyrosine kinase inhibitor with a high degree of specificity for the BCRABL, KIT, and platelet-derived growth factor receptor tyrosine kinases. It is thought that inhibition of platelet-derived growth factor receptor results in dis...

To date, 240 cases of bone marrow necrosis have been reported, of which only 13 were reported in association with chronic myelogenous leukemia (CML). Imatinib mesylate is an agent which can specifically inhibit the activity of tyrosine kinase chimeric protein BCR-ABL which is caused by the balanced translocation between the short arm of chromosome 9, and the long arm of chromosome 22, and is cl...

Mutational analysis of the c-kit gene in a patient with a previously undescribed variant of mast cell disease revealed a germline mutation, Phe522Cys, within the transmembrane portion of the Kit receptor protein. Transfection experiments revealed that the mutation caused ligand-independent autophosphorylation of Kit, which was inhibited by the tyrosine kinase inhibitor imatinib mesylate. The pa...

Chronic myeloid leukemia (CML) is a rare disease in children, accounting for 2%-3% of leukemias in this age group. Current treatment options of CML include tyrosine kinase inhibitors (TKIs) and allogeneic hematopoietic stem cell transplantation (HSCT) for children. Allogeneic HSCT has been recommended following attainment of remission with TKIs. Since long-term outcome and adverse effects of TK...

Imatinib mesylate is an effective, small-molecule, selective tyrosine kinase inhibitor, which inhibits BCR-ABL in patients with chronic myeloid leukemia, c-kit gastrointestinal tumor (GIST), and platelet-derived growth factors hypereosinophilic syndrome. Above all, bone marrow necrosis a rare complication of imatinib usage. If newly developed increased opacity lesions are seen metastatic GIST, ...