Celon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, Poland.
Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kiełpin, 05-092, Łomianki, Poland.
J Pharmacol Sci. 2021 Apr;145(4):340-348. doi: 10.1016/j.jphs.2021.02.002. Epub 2021 Feb 9.
Systemic lupus erythematosus is a chronic inflammatory disease, in which treatment is still limited due to suboptimal efficacy and toxicities associated with the available therapies. JAK kinases are well known to play an important role in systemic lupus erythematous. There is growing evidence that ROCK kinases are also important in disease development. In this paper, we present the results of the development of CPL409116, a dual JAK and ROCK inhibitor. The studies we performed demonstrate that this molecule is an effective JAK and ROCK inhibitor which efficiently blocks disease progression in NZBWF1/J mouse models of systemic lupus erythematous.
系统性红斑狼疮是一种慢性炎症性疾病，由于现有治疗方法的疗效不佳和毒性，其治疗仍然受到限制。JAK 激酶在系统性红斑狼疮中起着重要作用。越来越多的证据表明 ROCK 激酶在疾病发展中也很重要。本文介绍了双重 JAK 和 ROCK 抑制剂 CPL409116 的开发结果。我们进行的研究表明，该分子是一种有效的 JAK 和 ROCK 抑制剂，可有效阻止 NZBWF1/J 小鼠系统性红斑狼疮模型中的疾病进展。
