JAK inhibition reduces SARS-CoV-2 liver infectivity and modulates inflammatory responses to reduce morbidity and mortality.
Justin StebbingGinés Sánchez NievasMarco FalconeSonia YouhannaPeter RichardsonSilvia OttavianiJoanne X ShenChristian SommerauerGiusy TiseoLorenzo GhiadoniAgostino VirdisFabio MonzaniLuis Romero RizosFrancesco ForforiAlmudena Avendaño CéspedesSalvatore De MarcoLaura CarrozziFabio LenaPedro Manuel Sánchez-JuradoLeonardo Gianluca LacerenzaNencioni CesiraDavid Caldevilla BernardoAntonio PerrellaLaura NiccoliLourdes Sáez MéndezDaniela MatarreseDelia GolettiYee Joo TanVanessa M MonteilGeorge DranitsarisFabrizio CantiniAlessio FarcomeniShuchismita DuttaStephen K BurleyMirjana JerkicMauro PistelloWilliam LiMarta Mas RomeroFernando Andrés PretelRafaela Sánchez Simón-TaleroRafael García-MolinaClaudia KutterJames H FelceZehra F NizamiAndras G MiklosiJosef M PenningerFrancesco MenichettiAli MirazimiPedro Abizanda SolerVolker Martin LauschkePublished in: Science advances (2021)
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.
Keyphrases
- sars cov
- drug induced
- rna seq
- induced apoptosis
- liver injury
- respiratory syndrome coronavirus
- cell cycle arrest
- single cell
- randomized controlled trial
- genome wide
- poor prognosis
- immune response
- systematic review
- skeletal muscle
- risk factors
- coronary artery disease
- electronic health record
- copy number
- cell death
- high throughput
- type diabetes
- coronavirus disease
- cardiovascular disease
- angiotensin ii
- early onset
- middle aged
- binding protein
- artificial intelligence
- adverse drug
- acute respiratory distress syndrome
- transcription factor
- meta analyses