Minami Yosuke, Naoe Tomoki
Department of Hematology and Oncology, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Gan To Kagaku Ryoho. 2009 Apr;36(4):544-7.
In the emergence of resistance to imatinib, ABL-kinase inhibitor has become a significant problem despite the remarkable clinical results achieved with this drug in the treatment of chronic myeloid leukemia. The most common cause of imatinib resistance is the selection of leukemic clones with point mutation in the ABL-kinase domain. Persistent disease is another therapeutic challenge and may in part, be due to the inability of imatinib to eradicate primitive stem cell progenitors. A multitude of novel agents have been developed and shown efficacy in overcoming imatinib resistance.
尽管伊马替尼在治疗慢性髓性白血病方面取得了显著的临床效果,但对其产生耐药性已成为一个重大问题。伊马替尼耐药最常见的原因是选择了ABL激酶结构域发生点突变的白血病克隆。持续性疾病是另一个治疗挑战,部分原因可能是伊马替尼无法根除原始干细胞祖细胞。已经开发出多种新型药物,并显示出克服伊马替尼耐药性的疗效。