伊马替尼治疗慢性粒细胞白血病耐药机制及相关药物作用进展  

Mechanism of Resistance to Imatinib in Chronic Myelogenous Leukemia Treatment and Related Drug Development

作　　者：程雅馨 朱薇波[1] 

机构地区：[1]安徽医科大学附属省立医院血液科

出　　处：《医学综述》2016年第2期313-318,共6页Medical Recapitulate

摘　　要：伊马替尼,作为治疗慢性粒细胞白血病(CML)的一线药物,近年来因基因突变导致的临床耐药病例屡被报道。而第二代酪氨酸激酶抑制剂(TKIs),如尼洛替尼、达沙替尼,虽然对大部分突变型有效,但均对T315I突变反应不佳,这无疑成为CML治疗的最大挑战。该文就TKIs的作用机制及临床疗效进行阐述,并介绍尚在研究中对T315I突变型有效的药物。Imatinib, as a first-line treatment for chronic myeloid leukemia （CML）, has been frequently reported about resistance to the drug. Second generation of tyrosine kinase inhibitors （ TKIs）, such as dasatinib and nilotinib, are effective for several mutations, but do not respond well to T315I mutation, which became the greatest challenge to CML treatment. Here is to elaborate the clinical effect and mechanism of action of TKIs, and introduce possibly effective drugs still under study for T315I mutant.

关 键 词：慢性粒细胞白血病 酪氨酸激酶抑制剂 T315I AURORA激酶抑制剂 AP24534 

分 类 号：R55[医药卫生—血液循环系统疾病]