Department of Hematology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1095# Jiefang Ave., Wuhan 430030, People's Republic of China.
Department of Cardiology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1095# Jiefang Ave., Wuhan 430030, People's Republic of China.
Biochem Pharmacol. 2022 Aug;202:115162. doi: 10.1016/j.bcp.2022.115162. Epub 2022 Jul 3.
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) epidemic continues to spread globally. The rapid dispersion of coronavirus disease 2019 (COVID-19) caused by SARS-CoV-2 drives an urgent need for effective treatments, especially for patients who develop severe pneumonia. The excessive and uncontrolled release of pro-inflammatory cytokines has proved to be an essential factor in the rapidity of disease progression, and some cytokines are significantly associated with adverse outcomes. Most of the upregulated cytokines signal through the Janus kinase-signal transducer and activator of transcription (JAK/STAT) pathway. Therefore, blocking the exaggerated release of cytokines, including IL-2, IL-6, TNF-α, and IFNα/β/γ, by inhibiting JAK/STAT signaling will, presumably, offer favorable pharmacodynamics and present an attractive prospect. JAK inhibitors (JAKi) can also inhibit members of the numb-associated kinase (NAK) family, including AP2-associated kinase 1 (AAK1) and cyclin G-associated kinase (GAK), which regulate the angiotensin-converting enzyme 2 (ACE-2) transmembrane protein and are involved in host viral endocytosis. According to the data released from current clinical trials, JAKi treatment can effectively control the dysregulated cytokine storm and improve clinical outcomes regarding mortality, ICU admission, and discharge. There are still some concerns surrounding thromboembolic events, opportunistic infection such as herpes zoster virus reactivation, and repression of the host's type-I IFN-dependent immune repair for both viral and bacterial infection. However, the current JAKi clinical trials of COVID-19 raised no new safety concerns except a slightly increased risk of herpes virus infection. In the updated WHO guideline, Baricitinb is strongly recommended as an alternative to IL-6 receptor blockers, particularly in combination with corticosteroids, in patients with severe or critical COVID-19. Future studies will explore the application of JAKi to COVID-19 treatment in greater detail, such as the optimal timing and course of JAKi treatment, individualized medication strategies based on pharmacogenomics, and the effect of combined medications.
严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)的疫情在全球范围内持续蔓延。由 SARS-CoV-2 引起的 2019 年冠状病毒病(COVID-19)的快速传播导致人们迫切需要有效的治疗方法,特别是对那些患有严重肺炎的患者。大量失控的促炎细胞因子的释放被证明是疾病快速进展的一个重要因素,其中一些细胞因子与不良预后显著相关。大多数上调的细胞因子通过 Janus 激酶-信号转导和转录激活因子(JAK/STAT)途径发出信号。因此,通过抑制 JAK/STAT 信号来阻断细胞因子(包括 IL-2、IL-6、TNF-α和 IFNα/β/γ)的过度释放,可能会产生有利的药效学并呈现出诱人的前景。JAK 抑制剂(JAKi)还可以抑制 nummular 相关激酶(NAK)家族的成员,包括与 AP2 相关的激酶 1(AAK1)和与细胞周期蛋白 G 相关的激酶(GAK),它们调节血管紧张素转化酶 2(ACE-2)跨膜蛋白,并参与宿主病毒内吞作用。根据当前临床试验公布的数据,JAKi 治疗可以有效控制失调的细胞因子风暴,并改善死亡率、入住 ICU 和出院等临床结局。关于血栓栓塞事件、机会性感染(如疱疹病毒再激活)以及对宿主 I 型 IFN 依赖性抗病毒和细菌感染免疫修复的抑制,仍存在一些担忧。然而,目前 COVID-19 的 JAKi 临床试验除了疱疹病毒感染风险略有增加外,没有出现新的安全性问题。在世界卫生组织更新的指南中,强烈建议将巴瑞替尼作为 IL-6 受体阻滞剂的替代药物,特别是在 COVID-19 重症或危重症患者中与皮质类固醇联合使用。未来的研究将更详细地探讨 JAKi 在 COVID-19 治疗中的应用,例如 JAKi 治疗的最佳时机和疗程、基于药物基因组学的个体化用药策略以及联合用药的效果。