Ben Ami Eytan, Demetri George D
a Center for Sarcoma and Bone Oncology , Dana Farber Cancer Institute , Boston , MA , USA.
b Center for Sarcoma and Bone Oncology and Ludwig Center at Harvard , Dana-Farber Cancer Institute and Harvard Medical School , Boston , MA , USA.
Expert Opin Drug Saf. 2016;15(4):571-8. doi: 10.1517/14740338.2016.1152258. Epub 2016 Feb 27.
For the last 15 years, imatinib mesylate has been the first line treatment of choice for advanced (metastatic) GIST.
This review describes key efficacy data on imatinib for the treatment of GIST, and focuses on safety and tolerability of imatinib, with emphasis on common adverse events management and long term toxicity profile.
Imatinib has been the standard of care for metastatic GIST and probably will continue to be so for the next few years. Still, despite dramatic responses initially, imatinib drug resistance continues to be the major factor for treatment discontinuation. The toxicity profile of imatinib has been well characterized, and although the majority of patients experience an adverse event during treatment with imatinib, these side effects are usually mild and manageable, with the majority of patients continuing treatment uninterruptedly. Early concerns regarding imatinib related cardiotoxicity in GIST have not been confirmed in large prospective randomized trials, with reports indicating a low incidence of approximately 0.2%-0.4%. Future strategies for treatment of imatinib resistant GIST will probably include novel tyrosine kinase inhibitors, combination therapies or immunotherapy.
在过去15年中，甲磺酸伊马替尼一直是晚期（转移性）胃肠道间质瘤（GIST）的一线治疗选择。
本综述描述了伊马替尼治疗GIST的关键疗效数据，并重点关注伊马替尼的安全性和耐受性，着重介绍常见不良事件的管理及长期毒性特征。
伊马替尼一直是转移性GIST的治疗标准，未来几年可能仍将如此。尽管最初反应显著，但伊马替尼耐药性仍是导致治疗中断的主要因素。伊马替尼的毒性特征已得到充分描述，虽然大多数患者在接受伊马替尼治疗期间会出现不良事件，但这些副作用通常较轻且易于管理，大多数患者可继续不间断治疗。大型前瞻性随机试验未证实早期对GIST中伊马替尼相关心脏毒性的担忧，报告显示其发生率较低，约为0.2%-0.4%。未来治疗伊马替尼耐药GIST的策略可能包括新型酪氨酸激酶抑制剂、联合疗法或免疫疗法。
