イマチニブ 化學(xué)特性,用途語,生産方法
外観
白色～うすい黃色～うすい黃赤色粉末～結(jié)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(zhì)腫瘍などに対して使用される分子標(biāo)的治療薬。商品名グリベック。2001年にスイスの製薬會(huì)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(zhì)や、消化管間質(zhì)腫瘍の原因となる異常なKITたんぱく質(zhì)と結(jié)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(xì)胞や腫瘍の増殖を抑える。
小學(xué)館 デジタル大辭泉について 情報(bào) | 凡例
効能
抗悪性腫瘍薬, チロシンキナーゼ阻害薬
化學(xué)的特性
Orange Solid
使用
Imatinib impurity.
適応癥
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%
イマチニブ 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品