Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways

Objective To characterise the molecular pathways impacted by the pharmacologic effects of the Janus kinase (JAK) 1 and JAK2 inhibitor baricitinib in SLE.Methods In a phase II, 24-week, randomised, placebo-controlled, double-blind study (JAHH), RNA was isolated from whole blood in 274 patients and an...

Full description

Saved in:
Bibliographic Details
Main Authors: Daniel J Wallace, Thomas Dörner, Stephanie de Bono, Robert J Benschop, Ernst R Dow, Damiano Fantini, Richard E Higgs, Guilherme Rocha, Brenda Crowe, Nicole L Byers, Maria E Silk, Robert W Hoffman
Format: Article
Language:English
Published: BMJ Publishing Group 2020-10-01
Series:Lupus Science and Medicine
Online Access:https://lupus.bmj.com/content/7/1/e000424.full
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850257532049686528
author Daniel J Wallace
Thomas Dörner
Stephanie de Bono
Robert J Benschop
Ernst R Dow
Damiano Fantini
Richard E Higgs
Guilherme Rocha
Brenda Crowe
Nicole L Byers
Maria E Silk
Robert W Hoffman
author_facet Daniel J Wallace
Thomas Dörner
Stephanie de Bono
Robert J Benschop
Ernst R Dow
Damiano Fantini
Richard E Higgs
Guilherme Rocha
Brenda Crowe
Nicole L Byers
Maria E Silk
Robert W Hoffman
author_sort Daniel J Wallace
collection DOAJ
description Objective To characterise the molecular pathways impacted by the pharmacologic effects of the Janus kinase (JAK) 1 and JAK2 inhibitor baricitinib in SLE.Methods In a phase II, 24-week, randomised, placebo-controlled, double-blind study (JAHH), RNA was isolated from whole blood in 274 patients and analysed using Affymetrix HTA2.0 array. Serum cytokines were measured using ultrasensitive quantitative assays.Results Gene expression profiling demonstrated an elevation of STAT1, STAT2 and multiple interferon (IFN) responsive genes at baseline in patients with SLE. Statistical and gene network analyses demonstrated that baricitinib treatment reduced the mRNA expression of functionally interconnected genes involved in SLE including STAT1-target, STAT2-target and STAT4-target genes and multiple IFN responsive genes. At baseline, serum cytokines IFN-α, IFN-γ, interleukin (IL)-12p40 and IL-6 were measurable and elevated above healthy controls. Treatment with baricitinib significantly decreased serum IL-12p40 and IL-6 cytokine levels at week 12, which persisted through week 24.Conclusion Baricitinib treatment induced significant reduction in the RNA expression of a network of genes associated with the JAK/STAT pathway, cytokine signalling and SLE pathogenesis. Baricitinib consistently reduced serum levels of two key cytokines implicated in SLE pathogenesis, IL-12p40 and IL-6.
format Article
id doaj-art-e5cc766cafc64ce9bf61c760b2589fcd
institution OA Journals
issn 2053-8790
language English
publishDate 2020-10-01
publisher BMJ Publishing Group
record_format Article
series Lupus Science and Medicine
spelling doaj-art-e5cc766cafc64ce9bf61c760b2589fcd2025-08-20T01:56:24ZengBMJ Publishing GroupLupus Science and Medicine2053-87902020-10-017110.1136/lupus-2020-000424Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathwaysDaniel J Wallace0Thomas Dörner1Stephanie de Bono2Robert J Benschop3Ernst R Dow4Damiano Fantini5Richard E Higgs6Guilherme Rocha7Brenda Crowe8Nicole L Byers9Maria E Silk10Robert W Hoffman115Cedars-Sinai Medical Center/University California at Los Angeles, Los AngelesRheumatology and Clinical Immunology, Charite University Hospitals Berlin, Berlin, GermanyEli Lilly and Company, Indianapolis, Indiana, USALilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA6Eli Lilly and Company, Indianapolis, USA6Eli Lilly and Company, Indianapolis, USA5Eli Lilly and Company, Indianapolis, United States of America5Eli Lilly and Company, Indianapolis, United States of America6Eli Lilly and Company, Indianapolis, USA7 Eli Lilly and Company, Indianapolis, Indiana, USA6Eli Lilly and Company, Indianapolis, USA6Eli Lilly and Company, Indianapolis, USAObjective To characterise the molecular pathways impacted by the pharmacologic effects of the Janus kinase (JAK) 1 and JAK2 inhibitor baricitinib in SLE.Methods In a phase II, 24-week, randomised, placebo-controlled, double-blind study (JAHH), RNA was isolated from whole blood in 274 patients and analysed using Affymetrix HTA2.0 array. Serum cytokines were measured using ultrasensitive quantitative assays.Results Gene expression profiling demonstrated an elevation of STAT1, STAT2 and multiple interferon (IFN) responsive genes at baseline in patients with SLE. Statistical and gene network analyses demonstrated that baricitinib treatment reduced the mRNA expression of functionally interconnected genes involved in SLE including STAT1-target, STAT2-target and STAT4-target genes and multiple IFN responsive genes. At baseline, serum cytokines IFN-α, IFN-γ, interleukin (IL)-12p40 and IL-6 were measurable and elevated above healthy controls. Treatment with baricitinib significantly decreased serum IL-12p40 and IL-6 cytokine levels at week 12, which persisted through week 24.Conclusion Baricitinib treatment induced significant reduction in the RNA expression of a network of genes associated with the JAK/STAT pathway, cytokine signalling and SLE pathogenesis. Baricitinib consistently reduced serum levels of two key cytokines implicated in SLE pathogenesis, IL-12p40 and IL-6.https://lupus.bmj.com/content/7/1/e000424.full
spellingShingle Daniel J Wallace
Thomas Dörner
Stephanie de Bono
Robert J Benschop
Ernst R Dow
Damiano Fantini
Richard E Higgs
Guilherme Rocha
Brenda Crowe
Nicole L Byers
Maria E Silk
Robert W Hoffman
Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
Lupus Science and Medicine
title Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
title_full Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
title_fullStr Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
title_full_unstemmed Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
title_short Baricitinib-associated changes in global gene expression during a 24-week phase II clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune-related pathways
title_sort baricitinib associated changes in global gene expression during a 24 week phase ii clinical systemic lupus erythematosus trial implicates a mechanism of action through multiple immune related pathways
url https://lupus.bmj.com/content/7/1/e000424.full
work_keys_str_mv AT danieljwallace baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT thomasdorner baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT stephaniedebono baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT robertjbenschop baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT ernstrdow baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT damianofantini baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT richardehiggs baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT guilhermerocha baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT brendacrowe baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT nicolelbyers baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT mariaesilk baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways
AT robertwhoffman baricitinibassociatedchangesinglobalgeneexpressionduringa24weekphaseiiclinicalsystemiclupuserythematosustrialimplicatesamechanismofactionthroughmultipleimmunerelatedpathways