imatinib mesylate

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/04/18 15:59:40」(JST)

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英文文献

  • Major molecular response during the first year of dasatinib, imatinib or nilotinib treatment for newly diagnosed chronic myeloid leukemia: a network meta-analysis.
  • Signorovitch J, Ayyagari R, Reichmann WM, Wu EQ, Chen L.Author information Analysis Group, Inc., Boston, MA 02199, USA. Electronic address: jsignorovitch@analysisgroup.com.AbstractOBJECTIVE: No randomized trials have directly compared dasatinib with nilotinib for the treatment of newly diagnosed chronic myeloid leukemia in the chronic phase. The objective of this study was to indirectly compare these therapies using evidence from randomized trials versus imatinib, the current standard of care.
  • Cancer treatment reviews.Cancer Treat Rev.2014 Mar;40(2):285-92. doi: 10.1016/j.ctrv.2013.09.004. Epub 2013 Sep 17.
  • OBJECTIVE: No randomized trials have directly compared dasatinib with nilotinib for the treatment of newly diagnosed chronic myeloid leukemia in the chronic phase. The objective of this study was to indirectly compare these therapies using evidence from randomized trials versus imatinib, the current
  • PMID 24112812
  • Adherence to imatinib therapy in patients with gastrointestinal stromal tumors.
  • Blay JY, Rutkowski P.Author information Department of Medicine, Centre Léon-Bérard-Claude-Bernard Lyon-1 University, Lyon, France. Electronic address: jean-yves.blay@lyon.unicancer.fr.AbstractImatinib mesylate, an oral tyrosine kinase inhibitor, is indicated for first-line treatment of patients with unresectable and/or metastatic gastrointestinal stromal tumors (GIST). Imatinib also is approved as adjuvant therapy for patients following resection of primary GIST. Despite the efficacy of imatinib for the treatment of patients with GIST, adherence to treatment can prove difficult. Clinical studies have identified a number of factors that have a significant association with non-adherence to therapy, including age >51years, female sex, a high number of concomitant medications, and complications with patients' therapy or the disease itself. Moreover, treatment-related adverse events and increased healthcare costs have been shown to have an impact on patients' adherence to therapy. A study of perceptions of adherence to therapy found discrepancies between actual and perceived adherence rates; both patients and physicians overestimate adherence to treatment. Non-adherence to treatment is not exclusive to oncology, and occurs in other disease areas, particularly with chronic conditions. Evidence from other disease areas suggests that routine assessment of adherence and the implementation of adherence programs can lead to improvements in health status and reduced healthcare costs. Improving patient adherence to imatinib treatment for patients with unresectable/metastatic GIST is particularly important, because non-adherence has a significant impact on clinical outcomes and healthcare costs. Therefore, the effective management of treatment-related adverse events along with patient education may be important in keeping patients compliant with continuous therapy.
  • Cancer treatment reviews.Cancer Treat Rev.2014 Mar;40(2):242-7. doi: 10.1016/j.ctrv.2013.07.005. Epub 2013 Aug 7.
  • Imatinib mesylate, an oral tyrosine kinase inhibitor, is indicated for first-line treatment of patients with unresectable and/or metastatic gastrointestinal stromal tumors (GIST). Imatinib also is approved as adjuvant therapy for patients following resection of primary GIST. Despite the efficacy of
  • PMID 23931926
  • Bcr-Abl activates AURKA and AURKB in chronic myeloid leukemia cells via AKT signaling.
  • Yang J, Ikezoe T, Nishioka C, Udaka K, Yokoyama A.Author information Department of Hematology and Respiratory Medicine, Kochi University, Nankoku, Kochi, Japan; Department of Immunology, Kochi Medical School, Kochi University, Kochi University, Nankoku, Kochi, Japan.AbstractThis study explored molecular mechanisms by which Bcr-Abl induced expression of Aurora kinase A and B (AURKA and AURKB) in chronic myeloid leukemia cells. Lentiviral transduction of Bcr-Abl into either Ba/F3 or CD34(+) hematopoietic stem/progenitor cells potently increased levels of AURKA and AURKB in association with phosphorylation of AKT and stimulated their proliferation. Bcr-Abl-mediated expression of AURKA and AURKB were decreased in CD34(+) HSPCs when AKT was inactivated by an shRNA against AKT, suggesting that Bcr-Abl induced expression of AURKA and AURKB via AKT signaling. MLN8237, an inhibitor of AURKA, significantly inhibited the proliferation of freshly isolated CD34(+) CML cells in a dose-dependent manner as measured by colony forming assay. Importantly, inhibition of AURKA in CD34(+) leukemia cells freshly isolated from individuals with blast crisis of CML with Bcr-Abl T315I mutant (n = 2) by MLN8237 significantly impaired the engraftment of these cells in severely immunocompromised mice and decreased the weight of spleens. Taken together, Bcr-Abl induces expression of AURKA and AURKB at least in part via AKT. Inhibition of AURKA could be useful to overcome imatinib-resistance mediated by Bcr-Abl mutants.
  • International journal of cancer. Journal international du cancer.Int J Cancer.2014 Mar 1;134(5):1183-94. doi: 10.1002/ijc.28434. Epub 2013 Sep 3.
  • This study explored molecular mechanisms by which Bcr-Abl induced expression of Aurora kinase A and B (AURKA and AURKB) in chronic myeloid leukemia cells. Lentiviral transduction of Bcr-Abl into either Ba/F3 or CD34(+) hematopoietic stem/progenitor cells potently increased levels of AURKA and AURKB
  • PMID 23934627

和文文献

  • Imatinib Responsiveness in Canine Mast Cell Tumors Carrying Novel Mutations of c-KIT Exon 11
  • NAKANO Yuko,KOBAYASHI Tetsuya,OSHIMA Fukiko [他]
  • The journal of veterinary medical science 76(4), 545-548, 2014-04
  • NAID 40020088027
  • 症例報告 メチル酸イマチニブによる分子遺伝学的大寛解後に真性赤血球増加症を併発した慢性骨髄性白血病
  • 定免 渉,黒田 裕行,吉田 正宏 [他]
  • 臨床血液 55(3), 360-365, 2014-03
  • NAID 40020038366
  • 症例 イマチニブメシル酸塩にて治療効果が得られた隆起性皮膚線維肉腫肺転移の1例
  • 古堅 誠,仲松 正司,熱海 恵理子 [他]
  • 日本呼吸器学会誌 = Annals of the Japanese Respiratory Society 3(1), 107-110, 2014-01-10
  • NAID 40019962367

関連リンク

It is marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia/Latin America) as its mesylate salt, imatinib mesilate ... One study demonstrated that imatinib mesylate was effective in patients with systemic mastocytosis, including those ...

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★リンクテーブル★
リンク元イマチニブ」「STI-575
関連記事mesylate

イマチニブ」

  [★]

imatinib
imatinib mesylate
グリベック
nib
分子標的薬剤

分類

  • その他
  • チロシンキナーゼ阻害薬

特徴

構造

作用機序

  • ABLや、活性複合体であるv-ABL, BCR-ABL, [EVT6]-ABLを阻害する (GOO.1367)
  • (そのほかに)PDGFRとKITに対しても競合阻害作用を持つ (GOO.1367)
KITはgastrointestinal stromal tumor(GIST)と関連
ETV6-PDGFRはchronic myelomonocytic leukemia(CMML)と関連
FIP1L1-PDGFRAはhypereosinophilic syndrome(HES)と関連

薬理作用

動態

  • 経口投与

適応

グリベック錠100mg

  • 1. 慢性骨髄性白血病
  • 2. KIT陽性消化管間質腫瘍
  • 3. フィラデルフィア染色体陽性急性リンパ性白血病

注意

禁忌

副作用

相互作用

類似薬

添付文書

  • グリベック錠100mg
[display]http://www.info.pmda.go.jp/go/pack/4291011F1028_1_11/4291011F1028_1_11?view=body




STI-575」

  [★]

imatinib mesylate


mesylate」

  [★]

mesilatemethanesulfonate




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