摘要
伊马替尼作为第一代酪氨酸激酶抑制剂,已成功用于慢性粒细胞白血病慢性期的一线治疗,但耐药现象的出现,极大影响了伊马替尼的长期治疗效果。伊马替尼耐药机制复杂多样,大致归为两大类:依赖于BCR-ABL激酶活性的耐药机制和不依赖于BCR-ABL激酶活性的耐药机制。针对不同的耐药机制,人们提出了很多解决伊马替尼耐药性的方法,包括对新型酪氨酸激酶抑制剂的研究,联合下游信号通路抑制剂,以及对慢性粒细胞白血病干细胞的靶向用药等。
Imatinib, developed as the first molecularly targeted therapy that specifically inhibits the BCRABL tyrosine kinase, has been used for the first- line treatment for newly diagnosed chronic myeloid leukemia （CML） with its excellent hematologic and cytogenetic responses, particularly in patients with chronic phase CML. Nevertheless, the emergence of drug- resistance significantly affects the long- term therapeutic effects of imatinib. Various mechanisms were postulated for imatinib resistance, which can be broadly divided into BCR-ABL-dependent and BCR-ABL-independent mechanisms. More and more efforts have been focused on imatinib resistance such as new kinase inhibitors, targeting pathways downstream of BCR-ABL, and eradicating CML stem cells.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2013年第7期512-520,共9页
Chinese Journal of New Drugs and Clinical Remedies
基金
教育部留学回国人员科研启动基金资助项目
关键词
伊马替尼
抗药性
肿瘤
白血病
髓样
慢性
imatinib
drug resistance, neoplasm
leukemia, myeloid, chronic
