Onozawa Yusuke, Terashima Masanori
Division of Clinical Oncology, Shizuoka Cancer Center.
Gan To Kagaku Ryoho. 2011 May;38(5):738-43.
After the introduction of imatinib, the outcome for patients with advanced gastro-intestinal stromal tumor (GIST) was vastly improved. However, resistance to imatinib has become a new problem. The cause of resistance to imatinib is the low sensitivity of gene mutations in the KIT gene or PDGFRα, or an acquisition of additional mutations, and a low plasma level of imatinib. Sunitinib is the first drug that showed an effectiveness for treating GIST refractory to imatinib. New molecular target drugs for overcoming imatinib resistance are being developed now.
伊马替尼应用后，晚期胃肠道间质瘤（GIST）患者的预后得到了极大改善。然而，对伊马替尼耐药已成为一个新问题。伊马替尼耐药的原因是KIT基因或PDGFRα基因突变敏感性低、获得额外突变以及伊马替尼血浆水平低。舒尼替尼是首个对伊马替尼难治性GIST显示出疗效的药物。目前正在研发克服伊马替尼耐药的新型分子靶向药物。
