This study explored drug transporter expression levels and their impact on clinical response to imatinib and second-generation tyrosine kinase inhibitors (TKIs) in imatinib- resistant chronic myeloid leukemia (CML). Imatinib-resistant chronic phase CML patients treated with dasatinib (n=10) and nilotinib (n=12) were enrolled. The mRNA expression of the OCT-1, ABCG2, and ABCB1 genes was quantifi...

Cancer is a major global problem and is the second leading cause of mortality in the developed countries.Resistance to current chemotherapeutics and high incidence of adverse effects are the two principal reasons for developing new anticancer agents. Phenylacetamide derivatives can act as potential anticancer agents. Synthesis and screening of 2-(4-Fluorophenyl)-N-phenylacetamide derivatives in...

Purpose: Imatinib (Glivec) is a potent inhibitor of bcr/ abl, an oncogenic fusion protein that causes chronic myelogenous leukemia (CML). 1 acid glycoprotein (AGP) binds to imatinib with high affinity and inhibits imatinib activity in vitro and in vivo in an animal model. A pharmacokinetics analysis of imatinib was undertaken in CML patients. Experimental Design: Imatinib plasma concentrations ...

Cancer is a major global problem and is the second leading cause of mortality in the developed countries.Resistance to current chemotherapeutics and high incidence of adverse effects are the two principal reasons for developing new anticancer agents. Phenylacetamide derivatives can act as potential anticancer agents. Synthesis and screening of 2-(4-Fluorophenyl)-N-phenylacetamide derivatives in...

Introduction: chronic myeloid leukemia is one of the major diseases, which cause death worldwide. Tyrosine kinase responsible for uncontrolled cell growth and block its function. Its inhibition a promising route to control out grow cells. The purpose our study involves docking human Abl with seven ciprofloxacin derivatives comparison results free energy binding positive (Imatinib).Methods: pres...

PURPOSE Imatinib (Glivec) is a potent inhibitor of bcr/abl, an oncogenic fusion protein that causes chronic myelogenous leukemia (CML). alpha1 acid glycoprotein (AGP) binds to imatinib with high affinity and inhibits imatinib activity in vitro and in vivo in an animal model. A pharmacokinetics analysis of imatinib was undertaken in CML patients. EXPERIMENTAL DESIGN Imatinib plasma concentrati...

Recent data suggest that the role of CYP3A4 in imatinib metabolism is smaller than presumed. This study aimed to evaluate the quantitative importance of different cytochrome P450 (P450) enzymes in imatinib pharmacokinetics. First, the metabolism of imatinib was investigated using recombinant P450 enzymes and human liver microsomes with P450 isoform-selective inhibitors. Thereafter, an in silico...

Background and Aims: Detection of overexpression in tumor-inhibiting genes provides valuable information for leukemia diagnosis and prognosis. Chronic myeloid leukemia (CML) is a stem cell disorder determined by a well-defined genetic anomaly involving BCR-ABL translocation in the Philadelphia chromosome. Curcumin is a chemo-preventive agent for the primary cancer targets, such as the breast, p...

  Introduction: Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal neoplasms of the gastrointestinal tract. GIST has been shown to over-express c-KIT (CD117), the receptor tyrosine kinase. Imatinib (STI571 or Glivec) is a new type of tyrosine kinase inhibitor that selectively inhibits various tyrosine kinases and has been successfully used to trea...

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, ...