イマチニブ

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

イマチニブ 価格

イマチニブ 化学特性,用途語,生産方法

• 外観

  白色～うすい黄色～うすい黄赤色粉末～結晶

• 解説

  イマチニブ,抗癌剤(こうがんざい)の一つ。慢性骨髄性白血病・消化管間質腫瘍などに対して使用される分子標的治療薬。商品名グリベック。2001年にスイスの製薬会社ノバルティスファーマが発売。慢性骨髄性白血病の原因となるBCR-ABLという異常なたんぱく質や、消化管間質腫瘍の原因となる異常なKITたんぱく質と結びつく特定のチロシンキナーゼの働きを阻害することによって、骨髄造血幹細胞や腫瘍の増殖を抑える。

  小学館 デジタル大辞泉について　情報 | 凡例
  

• 効能

  抗悪性腫瘍薬, チロシンキナーゼ阻害薬

• 化学的特性

  Orange Solid

• 使用

  Imatinib impurity.

• 使用

  Targeting constitutive BCR::ABL1 kinase activity with tyrosine kinase inhibitors (TKIs), beginning with imatinib, has transformed CML management and substantially improved long-term survival.^[2]

• 適応症

  Bcr-Abl inhibitor imatinib (Gleevec(R), Novartis) was approved in 2001 by the FDA. Although fasudil was approved in 1995, imatinib is widely perceived as the first approved SMKI mainly owing to the fact that fasudil's kinase inhibitory mechanism was unknown at the time of approval, and efforts to gain approval of fasudil have been unsuccessful in the United States and Europe.
  The field of kinase inhibitor development has evolved rapidly since the approval of imatinib. Some of the key discoveries and events include (i) the discovery of MAPK/ERK inhibitors, for example, CI-1040 (PD184352), as the first series of type III inhibitors in 2003; (ii) the approval of first dual tyrosine kinase and serine/threonine kinase inhibitor sorafenib in 2005; (iii) the description of the first series of allosteric type IVkinase inhibitor, that is,GNF-2 and analogues that inhibit Bcr–Abl through an allosteric non-ATP-competitivemode, by Gray and coworkers in 2006; (iv) the approval of the first type III inhibitor trametinib in 2013; (v) the approval of the first covalent kinase inhibitors, afatinib and ibrutinib, in 2013; and (vi) the approval of the first lipid kinase inhibitor, that is, the PI3K inhibitor idelalisib, in 2014.
  By December 2016, kinase inhibitor drug discovery can leverage the structures of over 200 human kinases and 5000 kinases of all types, over 1 million publications, clinical data from more than 200 molecules currently in phase I–III trials, and post-marketing results from the approved 38 drugs.

• 一般的な説明

  non-receptor tyrosine kinase|
  Treatment: CML, ALL, GIST
  Oral bioavailability = 98%
  Elimination half-life = 20 h
  Protein binding = 95%

• 合成

  Cuiling Wang and colleagues reported a method for imatinib synthesis[1]. It is described by using the C–N coupling reaction of 4-(4-methylpiperazine-1-methyl)benzamide with N-(5-bromo-2-tolyl)-4-(3-pyridyl)pyrimidin-2-amine to form imatinib. In this synthetic route, the high efficiency and high selectivity of nano-ZnO as a catalyst is key to the mild hydrolysis of 4-(4-methylpiperazine-1-methyl)benzonitrile into the corresponding amide. The total imatinib yield was 51.3%, and the purity was 99.9%.
  

イマチニブ 上流と下流の製品情報

イマチニブ 生産企業

Global(694)Suppliers

イマチニブ スペクトルデータ(¹HNMR)

152459-95-5, イマチニブ キーワード