JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib

Selectivity of Janus Kinase Inhibitors in Rheumatoid Arthritis and Other Immune-Mediated Inflammatory Diseases: Is Expectation the Root of All Headache?

(2020) Masayoshi Harigai et al.   DRUGS

Janus kinases to jakinibs: from basic insights to clinical practice

(2019) Massimo Gadina et al.   RHEUMATOLOGY

Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I–III Clinical Trials

(2019) Ben Klünder et al.   CLINICAL PHARMACOKINETICS

Upadacitinib as monotherapy in patients with active rheumatoid arthritis and inadequate response to methotrexate (SELECT-MONOTHERAPY): a randomised, placebo-controlled, double-blind phase 3 study

(2019) Josef S Smolen et al.   LANCET

Effect of Filgotinib vs Placebo on Clinical Response in Patients With Moderate to Severe Rheumatoid Arthritis Refractory to Disease-Modifying Antirheumatic Drug Therapy

(2019) Mark C. Genovese et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain

(2019) James R. Burke et al.   Science Translational Medicine

Upadacitinib versus Placebo or Adalimumab in Patients with Rheumatoid Arthritis and an Inadequate Response to Methotrexate: Results of a Phase 3, Double‐Blind, Randomized Controlled Trial

(2019) Roy Fleischmann et al.   Arthritis & Rheumatology

The molecular details of cytokine signalling via the JAK/STAT pathway

(2018) Rhiannon Morris et al.   PROTEIN SCIENCE

The emerging safety profile of JAK inhibitors in rheumatic disease

(2017) Kevin L. Winthrop   Nature Reviews Rheumatology

Baricitinib versus Placebo or Adalimumab in Rheumatoid Arthritis

(2017) Peter C. Taylor et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Common Cytokine Receptor γ Chain Family of Cytokines

(2017) Jian-Xin Lin et al.   Cold Spring Harbor Perspectives in Biology

Filgotinib (GLPG0634/GS-6034), an oral selective JAK1 inhibitor, is effective as monotherapy in patients with active rheumatoid arthritis: results from a randomised, dose-finding study (DARWIN 2)

(2016) A Kavanaugh et al.   ANNALS OF THE RHEUMATIC DISEASES

Filgotinib (GLPG0634/GS-6034), an oral JAK1 selective inhibitor, is effective in combination with methotrexate (MTX) in patients with active rheumatoid arthritis and insufficient response to MTX: results from a randomised, dose-finding study (DARWIN 1)

(2016) R Westhovens et al.   ANNALS OF THE RHEUMATIC DISEASES

Baricitinib in Patients with Refractory Rheumatoid Arthritis

(2016) Mark C. Genovese et al.   NEW ENGLAND JOURNAL OF MEDICINE

The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention

(2015) John J. O'Shea et al.   Annual Review of Medicine

Therapeutic targets for rheumatoid arthritis: Progress and promises

(2014) Abdullah Alghasham et al.   AUTOIMMUNITY

Interleukin 6 and Rheumatoid Arthritis

(2014) Yuji Yoshida et al.   Biomed Research International

Janus kinase inhibitors in autoimmune diseases

(2013) John J O'Shea et al.   ANNALS OF THE RHEUMATIC DISEASES

Preclinical Characterization of GLPG0634, a Selective Inhibitor of JAK1, for the Treatment of Inflammatory Diseases

(2013) L. Van Rompaey et al.   JOURNAL OF IMMUNOLOGY

Conditional Deletion of Jak2 Reveals an Essential Role in Hematopoiesis throughout Mouse Ontogeny: Implications for Jak2 Inhibition in Humans

(2013) Sung O. Park et al.   PLoS One

JAK/STAT signaling in hematological malignancies

(2012) W Vainchenker et al.   ONCOGENE

JAK3 Specific Kinase Inhibitors: When Specificity Is Not Enough

(2011) Luk Cox et al.   CHEMISTRY & BIOLOGY

Jak1 Has a Dominant Role over Jak3 in Signal Transduction through γc-Containing Cytokine Receptors

(2011) Claude Haan et al.   CHEMISTRY & BIOLOGY

The type I IFN system in rheumatoid arthritis

(2010) Paola Conigliaro et al.   AUTOIMMUNITY

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

(2010) J. S. Fridman et al.   JOURNAL OF IMMUNOLOGY

Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis

(2010) Debra M Meyer et al.   Journal of Inflammation-London

Type I interferon in organ-targeted autoimmune and inflammatory diseases

(2010) Mary K Crow   ARTHRITIS RESEARCH & THERAPY

Cytokine Signaling Modules in Inflammatory Responses

(2008) John J. O'Shea et al.   IMMUNITY