Janus激酶1抑制剂PF-04965842

A Janus kinase 1 inhibitor: PF-04965842

Janus激酶(JAKs)是一类细胞内非受体酪氨酸激酶,介导多种细胞因子和生长因子的信号传导,参与免疫、炎症和造血细胞的发育、分化成熟、凋亡和功能表达等过程。JAK1在JAK家族成员中具有最广泛的细胞因子信号转导途径,JAK1选择性抑制剂可以抑制参与炎症和免疫功能的许多细胞因子,同时避免因抑制其他JAKs所引起的不良反应。PF-04965842是辉瑞公司正在开发的JAK1抑制剂,用于炎症性疾病的治疗。目前PF-04965842在中重度特异性皮炎治疗中的作用及与其他药物相互作用的影响研究正处于Ⅰ、Ⅱ、Ⅲ期临床研究中,其有效性和安全性已经得到验证。

Janus kinases(JAKs) are a family of intracellular non-receptor tyrosine kinases that mediate signal transduction of various cytokines and growth factors and are involved in immune, inflammatory, and hematopoietic cell development, differentiation, maturation, apoptosis, and functional expression. JAK1 has the broadest cytokine signaling profile among the JAK family members and is the only isoform that pairs with the other three JAKs. JAK1 selective inhibitors can inhibit many cytokines involved in inflammation and immune function, while avoiding adverse reactions caused by inhibition of other JAKs. PF-04965842 is a JAK1 inhibitor which is being developed by Pfizer for the treatment of inflammatory diseases. At present, the phase I, II, and III clinical trials of PF-04965842 in the treatment of moderate to severe atopic dermatitis and the effect of its interaction with other drugs are in progress and its effectiveness and safety have been confirmed.