• BMB Reports
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• v.38 no.6
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• pp.725-738
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• 2005

Resistance to imatinib mesylate (also known as Gleevec, Glivec, and STI571) often becomes a barrier to the treatment of chronic myelogenous leukemia (CML). In order to identify markers of the action of imatinib mesylate, we used a mass spectrometry approach to compare protein expression profiles in human leukemia cells (K562) and in imatinib mesylate-resistant human leukemia cells (K562-R) in the presence and absence of imatinib mesylate. We identified 118 differentially regulated proteins in these two leukemia cell-lines, with and without a $1\;{\mu}M$ imatinib mesylate challenge. Nine proteins of unknown function were discovered. This is the first comprehensive report regarding differential protein expression in imatinib mesylate-treated CML cells.

• Tuberculosis and Respiratory Diseases
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• v.59 no.4
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• pp.423-426
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• 2005

Imatinib-mesylate (Gleevec, Glivec) is a protein-tyrosine kinase inhibitor that inhibits the Bcr-Abl tyrosine kinase created by the Philadelphia chromosome abnormality in CML. Imatinib is also used to treat patients with c-kit (CD 117)-positive unresectable tumors, or metastatic malignant gastrointestinal stromal tumors, or both. Imatinib is a welltolerated drug with few side effects. However, it has been associated with gastrointestinal irritation, fluid retention and edema, skin rashes, depigmentation, hepatotoxicity, hemorrhage, and hematological toxicity (anemia, neutropenia, and thrombocytopenia). In addition, imatinib has been associated with dyspnea and cough, which are mainly secondary to the pleural effusion and pulmonary edema, which represent local or general fluid retention. These events appear to be dose related and are more common encountered in the elderly. However, there has been no report of hypersensitivity pneumonitis associated with imatinib-mesylate in Korea. We report a case of 51-year old woman who developed hypersensitivity pneumonitis that might have been induced by imatinib-mesylate during the treatment of a gastrointestinal stromal tumor.

• Journal of Yeungnam Medical Science
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• v.36 no.2
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• pp.155-158
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• 2019

Imatinib mesylate is currently used as the first-line treatment for metastatic gastrointestinal stromal tumors (GISTs). Imatinib-induced hepatotoxicity in patients with GIST is very rare. Its features vary from subclinical elevation of serum aminotransferase to clinically apparent acute hepatitis, which is associated with immunologic reactions. Imatinib-induced hepatotoxicity with autoimmune-like features can be treated by the discontinuation of imatinib mesylate and the administration of oral steroids. Here, we report a case of late-onset imatinib-induced hepatitis with autoimmune-like features in a patient with metastatic GIST, which was improved by oral corticosteroids.

• Journal of the Korean Chemical Society
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• v.55 no.3
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• pp.364-372
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• 2011

The corrosion inhibition of imatinib mesylate (IMT) on mild steel in 0.25 M sulphuric acid has been studied using gravimetric and potentiodynamic polarization techniques at various concentrations of inhibitor, temperature and fluid velocities. The results obtained showed that, inhibition efficiency (% IE) increases with increasing concentration of the inhibitor. The adsorption process on mild steel surface follows Langmuir adsorption isotherm. The values of Gibbs free energies of adsorption obtained suggest that, the adsorption process of IMT on mild steel is chemisorption. Thermodynamic parameters were evaluated and discussed. The electron orbital density distribution of HOMO and LUMO of IMT was used to discuss the inhibition mechanism. FT-IR spectroscopy and SEM images were used to analyze the surface adsorbed film.

• The Korean journal of helicobacter and upper gastrointestinal research
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• v.18 no.4
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• pp.264-270
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• 2018

Gastrointestinal stromal tumor (GIST) is a mesenchymal tumor derived from Cajal cells originating from the myotonic plexus. The expression of tyrosine kinase (KIT) membrane receptors that are active on KIT is inhibited by the KIT inhibitor imatinib mesylate. GISTs are resistant to conventional chemotherapy, and radiation therapy is not significantly beneficial for GISTs. With the development of imatinib mesylate, approximately 81.6% of patients with advanced and metastatic GIST exhibit an effect above the stabilization response, thereby increasing the survival time. However, imatinib mesylate alone is unlikely to cure metastatic GISTs. Even with a partial or stable response, imatinib mesylate may be used for a longer time period. However, resection of grossly visible lesions should be considered for patients with a stable response during surgical treatment. In this study, we present a case of GIST with liver metastasis after imatinib mesylate treatment, which was followed up without recurrence after partial resection.

• Tuberculosis and Respiratory Diseases
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• v.71 no.3
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• pp.210-215
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• 2011

Imatinib mesylate, a selective inhibitor of BCR-ABL kinase activity, has demonstrated significant clinical efficacy in the treatment of chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs). It has become the standard of treatment for these diseases. Although the toxicity profile of imatinib is superior to that of interferon or other cytotoxic agents, some adverse events including edema, gastrointestinal toxicities and hematologic toxicities are commonly observed in the patients treated by imatinib. We present two cases of imatinib induced interstitial pneumonitis during the treatment of a chronic phase of CML.

• Journal of Veterinary Clinics
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• v.34 no.6
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• pp.445-448
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• 2017

A 1.5-year-old neutered male domestic short hair cat was presented with multiple nodular mass, and suspected mast cell tumor on the surface of the right ear, accompanied by submandibular lymph node involvement. Histopathological Examinations and KIT (CD117) immunohistochemical staining was performed after the surgical resection of the entire right ear pinna. This patient was diagnosed with an anaplastic mast cell tumor with a diffuse positive cytoplasmic expression of KIT. Imatinib mesylate was prescribed after surgical resection; the patient presented without recurrence or metastasis for 2 years. Mild leukopenia was observed as the only side effect of imatinib mesylate during medication.

• Journal of Veterinary Clinics
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• v.34 no.2
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• pp.152-155
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• 2017

A 5-year-old intact female Maltese dog was referred to us with a history of left side head tilt and ataxia. Based on magnetic resonance imaging (MRI) and cerebrospinal fluid analysis results, the patient was tentatively diagnosed to meningoencephalitis of unknown etiology (MUE). Clinical signs were gradually improved and diminished after imatinib mesylate plus prednisolone therapy. At 90 days after treatment, we performed MRI recheck and brain inflammatory lesions were significantly improved compared with initial MRI results. However, the present patient showed head turn and tetraparesis after anesthesia and euthanized according to client's request. This report describes the clinical findings, serial magnetic resonance imaging characteristics under imatinib mesylate treatment in a MUE case.

• Tuberculosis and Respiratory Diseases
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• v.75 no.6
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• pp.256-259
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• 2013

Imatinib mesylate is a targeted therapy that acts by inhibiting tyrosine kinase of the bcr-abl fusion oncoprotein, which is specific to chronic myeloid leukemia (CML), and the c-transmembrane receptor, which is specific to gastrointestinal stromal tumors. Interstitial pneumonitis is a rare adverse event of imatinib therapy. It is clinically difficult to distinguish from infectious pneumonia, which can frequently occur due to the underlying disease. The standard treatment for imatinib-induced pneumonitis is to discontinue the medication and optionally administer corticosteroids. However, there are a few cases of successful retrial with imatinib. We describe a case of successful rechallenge of imatinib in a patient with imatinib-induced interstitial pneumonitis and CML without a recurrence of the underlying disease after 3 months of follow-up.

• Clinical and Experimental Pediatrics
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• v.56 no.8
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• pp.343-350
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• 2013

Purpose: Despite the established role of imatinib (IM) in chronic myelogenous leukemia (CML) in adults, there are few reports on its efficacy in children. In this study, we compared the outcomes of children with CML before and after the advent of IM-based treatment. Methods: The study cohort consisted of 52 patients treated for CML at the Department of Pediatrics, The Catholic University of Korea from January 1995 to October 2010. Patients were divided and analyzed according to the preImatinib group (pre-IMG) and imatinib group (IMG). Results: Median age at diagnosis for the overall cohort (pre-IMG, n=27; IMG, n=25) was 9 years, with a median follow-up duration of survivors of 84 months. Except for 5 patients in the IMG, all were diagnosed in chronic phase (CP). The overall survival (OS) of patients diagnosed in CP was 45.7% and 89.7% for pre-IMG and IMG, respectively (P=0.025). The OS of hematopoietic stem cell transplantation (HSCT) recipients in the 2 groups was similar, but the OS of patients diagnosed in CP who did not receive HSCT was superior in IMG (91.7% vs. 16.7%, P=0.014). Of the 12 patients in IMG who remained on IM without HSCT, 2 showed disease progression, compared to 11 of 12 in pre-IMG. No difference was observed in the progression free survival (PFS) of matched donor HSCT recipients and IM-based treatment recipients. Conclusion: Similar PFS of patients treated with IM and those who received matched donor HSCT underscore the potential of IM as effective first-line treatment in childhood CML.