Department of Surgery and Cancer, Imperial College, London, UK.
Department of Rheumatology, Complejo Hospitalario Universitario de Albacete, Albacete, Spain.
Sci Adv. 2021 Jan 1;7(1). doi: 10.1126/sciadv.abe4724. Print 2021 Jan.
Using AI, we identified baricitinib as having antiviral and anticytokine efficacy. We now show a 71% (95% CI 0.15 to 0.58) mortality benefit in 83 patients with moderate-severe SARS-CoV-2 pneumonia with few drug-induced adverse events, including a large elderly cohort (median age, 81 years). An additional 48 cases with mild-moderate pneumonia recovered uneventfully. Using organotypic 3D cultures of primary human liver cells, we demonstrate that interferon-α2 increases ACE2 expression and SARS-CoV-2 infectivity in parenchymal cells by greater than fivefold. RNA-seq reveals gene response signatures associated with platelet activation, fully inhibited by baricitinib. Using viral load quantifications and superresolution microscopy, we found that baricitinib exerts activity rapidly through the inhibition of host proteins (numb-associated kinases), uniquely among antivirals. This reveals mechanistic actions of a Janus kinase-1/2 inhibitor targeting viral entry, replication, and the cytokine storm and is associated with beneficial outcomes including in severely ill elderly patients, data that incentivize further randomized controlled trials.
利用人工智能,我们发现巴瑞替尼具有抗病毒和细胞因子抑制作用。我们现在在 83 名患有中度至重度 SARS-CoV-2 肺炎的患者中观察到 71%(95%CI 0.15 至 0.58)的死亡率降低,这些患者几乎没有药物引起的不良事件,包括一个大型老年队列(中位年龄 81 岁)。另外 48 例轻度至中度肺炎患者恢复顺利。利用原代人肝细胞的器官型 3D 培养物,我们证明干扰素-α2 通过增加 ACE2 的表达使实质细胞中 SARS-CoV-2 的感染性增加五倍以上。RNA-seq 揭示了与血小板激活相关的基因反应特征,巴瑞替尼可完全抑制这些特征。通过病毒载量定量和超分辨率显微镜,我们发现巴瑞替尼通过抑制宿主蛋白(与 NUMB 相关的激酶)迅速发挥作用,这在抗病毒药物中是独一无二的。这揭示了一种针对病毒进入、复制和细胞因子风暴的 Janus 激酶-1/2 抑制剂的作用机制,与包括重症老年患者在内的良好结果相关,这些数据鼓励进一步进行随机对照试验。