Department of Rheumatology, Hospital for Special Surgery, 535 East 70th Street, New York, NY 10021, USA.
Curr Rheumatol Rep. 2011 Feb;13(1):51-8. doi: 10.1007/s11926-010-0146-6.
Imatinib mesylate has become a therapy of interest for the treatment of systemic sclerosis because of its ability to inhibit c-Abl and platelet-derived growth factor receptor, tyrosine kinases involved in profibrotic pathways. Preclinical data using in vitro and murine models of fibrosis have demonstrated the antifibrotic properties of imatinib. Imatinib is currently used widely in the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors, and other conditions, and a large amount of information is available regarding the safety of the medication in these patient populations. Whether imatinib will be tolerable or effective in the treatment of systemic sclerosis is the subject of several investigations. The aim of this review is to summarize this body of research to date.
甲磺酸伊马替尼因其能够抑制酪氨酸激酶 c-Abl 和血小板衍生生长因子受体,而成为治疗系统性硬化症的研究热点,这些酪氨酸激酶参与了致纤维化途径。使用体外和纤维化的鼠模型的临床前数据已经证明了伊马替尼的抗纤维化特性。伊马替尼目前广泛用于治疗慢性髓性白血病、胃肠道间质瘤和其他疾病,并且有大量关于该药物在这些患者人群中的安全性的信息。伊马替尼在治疗系统性硬化症方面是否耐受或有效是几项研究的主题。本综述的目的是总结迄今为止这方面的研究。