BACKGROUND The functional activity of the organic cation transporter 1 (OCT-1) protein (OCT-1 activity) is an excellent predictor of molecular response and progression-free survival in patients with newly diagnosed chronic phase chronic myeloid leukemia treated with imatinib as front-line therapy. DESIGN AND METHODS In this study the predictive value of OCT-1 activity in patients treated with...

In the present work high performance liquid chromatography method was developed and validated for imatinib mesylate its related substances. The analyzed active pharmaceutical ingredient impurities were separated by Atlantis T3 (150 mm×4.6 mm), 3 μm column with ultraviolet detection at 230 nm. mobile phase has been used in specific composition (50:50, v/v, organic inorganic) that prepared using ...

The BCR/ABL tyrosine kinase inhibitor imatinib mesylate is highly effective in the treatment of chronic myelogenous leukemia (CML) but fails to eliminate all leukemia cells. Residual leukemia stem and progenitor cells persist in imatinib-responsive patients and may be a potential source of relapse. Previous studies indicate that imatinib preferentially targets dividing cells, and nondividing pr...

Chronic myeloid leukemia (CML) cells express the active BCR-ABL1 protein, which has been targeted by imatinib in CML therapy, but resistance to this drug is an emerging problem. BCR-ABL1 induces endogenous oxidative stress promoting genomic instability and imatinib resistance. In the present work, we investigated the extent of oxidative stress, DNA damage, apoptosis and expression of apoptosis-...

Osteoclasts (OCs) are large multinucleated cells derived from progenitor cells of the monocyte-macrophage lineage. Signal transduction via the macrophage-colony-stimulating factor (M-CSF) receptor, c-fms, is essential for OC formation. Since we have previously demonstrated inhibition of c-fms by imatinib, we examined the effect of imatinib on OC formation and activity. OC formation was not affe...

Imatinib mesylate has shown remarkable efficacy in the treatment of patients in the chronic phase of chronic myeloid leukemia. However, despite an overall significant hematological and cytogenetic response, imatinib therapy may favor the emergence of drug-resistant clones, ultimately leading to relapse. Some imatinib resistance mechanisms had not been fully elucidated yet. In this study we used...

background: imatinib mesylate is the first generation of tyrosine kinase inhibitors (tki) and highly effective in the treatment of chronic myeloid leukemia (cml). we aimed to evaluate thyroid function at baseline and at 1, 3, 6 and 12 months after initiation of imatinib mesylate therapy in 20 newly diagnosed bcr-abl positive cml patients. methods: this study was done during 2013-2014, 20 new ca...

A survival benefit for imatinib mesylate versus interferon-alpha therapy could not be demonstrated in the randomized study in newly diagnosed Philadelphia chromosome (Ph)-positive chronic-phase chronic myelogenous leukemia (CML) due to the high rate of crossover (90%) from interferon-alpha to imatinib mesylate within a year of study entry. We compared survival in 279 patients with newly diagnos...

and in 72% of the imatinib arms (P = 0.0011); confirmed CCyRs were reported in 77% and 66% of patients in the two groups, respectively (P = 0.0067). An analysis of CCyR rates at 3, 6, 9, and 12 months revealed that the likelihood of achieving CCyRs at all points remained approximately 50% higher with dasatinib than with imatinib throughout the study (P < 0.001; hazard ratio [HR], –1.53). MMR ra...

Imatinib mesylate is remarkably effective in treating chronic myeloid leukemia and metastatic gastrointestinal stromal tumors. Meanwhile, anaplastic thyroid carcinoma (ATC) remains a fatal malignancy for which there are currently no effective curative interventions. In chronic myeloid leukemia and gastrointestinal stromal tumors, imatinib inhibits the constitutive tyrosine kinase activity of BC...