Azizi Gholamreza, Mirshafiey Abbas
Department of Immunology, School of Public Health, Tehran University of Medical Sciences, Tehran- 14155, Box: 6446, Iran.
Recent Pat Inflamm Allergy Drug Discov. 2013 Sep;7(3):259-67. doi: 10.2174/1872213x113079990021.
Imatinib mesylate is a selective protein tyrosine kinase inhibitor, which can inhibit BCR/Abl, PDGF-R, c-KIT, c-fms, TCR/Abl, Lck, FLT-3 and MAPKs activities on various cell types. On immune system, imatinib has antiproliferative activity and immunomodulatory effects in lymphocytes, macrophages, mast cells and dendritic cells with abrogating multiple signal transduction pathways involved in pathogenesis of autoimmune diseases e.g. inhibiting IFN-γ, TNF-α, IL-1β and IL-17 pro-inflammatory cytokines and MMPs secretion. To date, the efficacy of imatinib in numerous animal model of autoimmune diseases (rheumatoid arthritis, multiple sclerosis, autoimmune diabetes and glomerulonephritis) has been demonstrated, but application of this drug in human autoimmune diseases should be tested in future clinical trials. This review provides an update on the use of tyrosine kinase inhibitor imatinib mesylate in treatment of autoimmune diseases and its related recent patents that could be developed as a novel and available therapy for the management of the autoimmunity improvement.
甲磺酸伊马替尼是一种选择性蛋白酪氨酸激酶抑制剂，它可以抑制多种细胞类型上的BCR/Abl、PDGF-R、c-KIT、c-fms、TCR/Abl、Lck、FLT-3和MAPKs活性。在免疫系统方面，伊马替尼在淋巴细胞、巨噬细胞、肥大细胞和树突状细胞中具有抗增殖活性和免疫调节作用，可消除参与自身免疫性疾病发病机制的多种信号转导途径，例如抑制IFN-γ、TNF-α、IL-1β和IL-17等促炎细胞因子以及MMPs的分泌。迄今为止，伊马替尼在众多自身免疫性疾病动物模型（类风湿性关节炎、多发性硬化症、自身免疫性糖尿病和肾小球肾炎）中的疗效已得到证实，但该药物在人类自身免疫性疾病中的应用有待未来临床试验检验。本综述提供了酪氨酸激酶抑制剂甲磺酸伊马替尼在自身免疫性疾病治疗中的应用最新情况及其相关近期专利，这些专利有望开发成为一种新型且可行的疗法，用于改善自身免疫。
