Department of Internal Medicine III, University of Erlangen-Nuremberg, Germany.
Am J Pathol. 2012 Nov;181(5):1672-80. doi: 10.1016/j.ajpath.2012.07.017. Epub 2012 Aug 31.
Chronic graft-versus-host disease (cGvHD) is a common complication of allogeneic bone marrow transplantation, and has a major effect on the long-term prognosis. The molecular mechanisms underlying cGvHD have been only partially revealed, and molecular targeted therapies have not yet been established for clinical use. We examined the effects of the combined inhibition of the Abelson kinase (c-Abl) and platelet-derived growth factor receptors (PDGFR) in experimental sclerodermatous cGvHD. Treatment using imatinib or nilotinib abolished the aberrant activation of c-Abl and PDGFR and protected against experimental cGvHD. Preventive therapy using imatinib or nilotinib inhibited the development of sclerodermatous cGvHD. Clinical features such as weight loss, alopecia, and skin ulcers, and histologic features with dermal thickening and accumulation of collagen were significantly reduced in mice that received imatinib or nilotinib therapy, but not in mice that received prednisone therapy. Of note, imatinib and nilotinib were also effective for treatment of experimental cGvHD that had already been clinically manifested. In summary, the combined inhibition of c-Abl and PDGFR is effective for prevention and treatment of experimental sclerodermatous cGvHD. Considering the high morbidity associated with cGvHD, the lack of efficient molecular therapies for clinical use, and first positive signals from uncontrolled studies of imatinib, combined inhibition of c-Abl and PDGFR might be a promising future strategy for treatment of sclerodermatous cGvHD.
慢性移植物抗宿主病(cGvHD)是异基因骨髓移植的常见并发症,对长期预后有重大影响。cGvHD 的分子机制仅部分揭示,且尚未确立用于临床的分子靶向治疗。我们研究了联合抑制 Abelson 激酶(c-Abl)和血小板衍生生长因子受体(PDGFR)对实验性硬皮病 cGvHD 的影响。使用伊马替尼或尼罗替尼治疗可消除 c-Abl 和 PDGFR 的异常激活,并可预防实验性 cGvHD。使用伊马替尼或尼罗替尼进行预防治疗可抑制硬皮病 cGvHD 的发展。接受伊马替尼或尼罗替尼治疗的小鼠体重减轻、脱发和皮肤溃疡以及皮肤增厚和胶原积累的组织学特征等临床特征明显减少,而接受泼尼松治疗的小鼠则没有。值得注意的是,伊马替尼和尼罗替尼对已经出现临床症状的实验性 cGvHD 也有效。总之,联合抑制 c-Abl 和 PDGFR 可有效预防和治疗实验性硬皮病 cGvHD。鉴于 cGvHD 的高发病率、缺乏有效的临床应用分子疗法以及伊马替尼的非对照研究的首次积极信号,联合抑制 c-Abl 和 PDGFR 可能是治疗硬皮病 cGvHD 的一种有前途的未来策略。