Small Molecule Inhibitors in the Treatment of Rheumatoid Arthritis and Beyond: Latest Updates and Potential Strategy for Fighting COVID-19

Efficacy of pharmacological treatment in rheumatoid arthritis: a systematic literature research informing the 2019 update of the EULAR recommendations for management of rheumatoid arthritis

(2020) Andreas Kerschbaumer et al.   ANNALS OF THE RHEUMATIC DISEASES

COVID-19: combining antiviral and anti-inflammatory treatments

(2020) Justin Stebbing et al.   LANCET INFECTIOUS DISEASES

Iguratimod as a New Drug for Rheumatoid Arthritis: Current Landscape

(2020) Sisi Xie et al.   Frontiers in Pharmacology

Clinical course of COVID-19 in a series of patients with chronic arthritis treated with immunosuppressive targeted therapies

(2020) Sara Monti et al.   ANNALS OF THE RHEUMATIC DISEASES

Characteristics associated with hospitalisation for COVID-19 in people with rheumatic disease: data from the COVID-19 Global Rheumatology Alliance physician-reported registry

(2020) Milena Gianfrancesco et al.   ANNALS OF THE RHEUMATIC DISEASES

COVID-19 infection and rheumatoid arthritis: Faraway, so close!

(2020) Ennio Giulio Favalli et al.   AUTOIMMUNITY REVIEWS

Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition

(2020) Albert Liclican et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor

(2020) Markus Hoffmann et al.   CELL

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders

(2020) Pengfei Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recommendations for coronavirus infection in rheumatic diseases treated with biologic therapy

(2020) Angela Ceribelli et al.   JOURNAL OF AUTOIMMUNITY

Baricitinib for COVID-19: a suitable treatment? – Authors' reply

(2020) Peter J Richardson et al.   LANCET INFECTIOUS DISEASES

Baricitinib for COVID-19: a suitable treatment?

(2020) Ennio G Favalli et al.   LANCET INFECTIOUS DISEASES

Efficacy and safety of upadacitinib in Japanese patients with rheumatoid arthritis (SELECT-SUNRISE): a placebo-controlled phase IIb/III study

(2020) Hideto Kameda et al.   RHEUMATOLOGY

Efficacy and Safety of PF‐06651600 (Ritlecitinib), a Novel JAK3/TEC Inhibitor in Patients with Moderate to Severe Rheumatoid Arthritis and an Inadequate Response to Methotrexate

(2020) Michael F. Robinson et al.   Arthritis & Rheumatology

HiJAKing SARS-CoV-2? The potential role of JAK inhibitors in the management of COVID-19

(2020) Francesca Romana Spinelli et al.   Science Immunology

Thromboembolic Safety Reporting of Tofacitinib and Baricitinib: An Analysis of the WHO VigiBase

(2020) Enriqueta Vallejo-Yagüe et al.   DRUG SAFETY

A rationale for blocking thromboinflammation in COVID-19 with Btk inhibitors

(2020) Phillip LR. Nicolson et al.   PLATELETS

Inhibition of Bruton tyrosine kinase in patients with severe COVID-19

(2020) Mark Roschewski et al.   Science Immunology

Selective Janus kinase inhibitors come of age

(2019) John J. O’Shea et al.   Nature Reviews Rheumatology

Cardiovascular Safety During Treatment with Baricitinib in Rheumatoid Arthritis

(2019) Peter C. Taylor et al.   Arthritis & Rheumatology

Tofacitinib in Combination with Methotrexate in Patients with Rheumatoid Arthritis: Clinical Efficacy, Radiographic and Safety Outcomes from the 24-Month Phase 3 ORAL Scan Study

(2019) Désirée van der Heijde et al.   Arthritis & Rheumatology

Janus kinases to jakinibs: from basic insights to clinical practice

(2019) Massimo Gadina et al.   RHEUMATOLOGY

Safety profile of baricitinib in Japanese patients with active rheumatoid arthritis with over 1.6 years median time in treatment: An integrated analysis of Phases 2 and 3 trials

(2019) Masayoshi Harigai et al.   Modern Rheumatology

Impact of Janus kinase inhibitors on risk of cardiovascular events in patients with rheumatoid arthritis: systematic review and meta-analysis of randomised controlled trials

(2019) Wenhui Xie et al.   ANNALS OF THE RHEUMATIC DISEASES

Rheumatoid arthritis (RA) and cardiovascular disease

(2019) Arnon Blum et al.   AUTOIMMUNITY REVIEWS

Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models

(2019) Philipp Haselmayer et al.   JOURNAL OF IMMUNOLOGY

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

JAK3-selective inhibitor peficitinib for the treatment of rheumatoid arthritis

(2019) Qian Qiu et al.   Expert Review of Clinical Pharmacology

Safety and effectiveness of upadacitinib or adalimumab plus methotrexate in patients with rheumatoid arthritis over 48 weeks with switch to alternate therapy in patients with insufficient response

(2019) Roy M Fleischmann et al.   ANNALS OF THE RHEUMATIC DISEASES

Efficacy and safety of peficitinib (ASP015K) in patients with rheumatoid arthritis and an inadequate response to conventional DMARDs: a randomised, double-blind, placebo-controlled phase III trial (RAJ3)

(2019) Yoshiya Tanaka et al.   ANNALS OF THE RHEUMATIC DISEASES

Efficacy and safety of peficitinib (ASP015K) in patients with rheumatoid arthritis and an inadequate response to methotrexate: results of a phase III randomised, double-blind, placebo-controlled trial (RAJ4) in Japan

(2019) Tsutomu Takeuchi et al.   ANNALS OF THE RHEUMATIC DISEASES

Exposure‐Response Analyses of Upadacitinib Efficacy in Phase 2 Trials in Rheumatoid Arthritis and Basis for Phase 3 Dose Selection

(2019) Mohamed‐Eslam F. Mohamed et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

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

Efficacy and safety of long-term baricitinib with and without methotrexate for the treatment of rheumatoid arthritis: experience with baricitinib monotherapy continuation or after switching from methotrexate monotherapy or baricitinib plus methotrexate

(2019) Roy Fleischmann et al.   ARTHRITIS CARE & RESEARCH

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

Patients with rheumatoid arthritis facing sick leave or work disability meet varying regulations: a study among rheumatologists and patients from 44 European countries

(2019) Polina Putrik et al.   ANNALS OF THE RHEUMATIC DISEASES

JAK inhibitors in 2019, synthetic review in 10 points

(2019) Romain Muller   European Journal of Internal Medicine

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

(2019) Richard D. Caldwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

The new entries in the therapeutic armamentarium: The small molecule JAK inhibitors

(2019) Katie Bechman et al.   PHARMACOLOGICAL RESEARCH

Effect of Baricitinib and Adalimumab in Reducing Pain and Improving Function in Patients with Rheumatoid Arthritis in Low Disease Activity: Exploratory Analyses from RA-BEAM

(2019) Bruno Fautrel et al.   Journal of Clinical Medicine

The Giants (biologicals) against the Pigmies (small molecules), pros and cons of two different approaches to the disease modifying treatment in rheumatoid arthritis

(2019) Ennio Giulio Favalli et al.   AUTOIMMUNITY REVIEWS

Development of Bruton’s tyrosine kinase Inhibitors for Rheumatoid Arthritis

(2018) Lv Jiahui et al.   CURRENT MEDICINAL CHEMISTRY

Safety and efficacy of upadacitinib in patients with active rheumatoid arthritis refractory to biologic disease-modifying anti-rheumatic drugs (SELECT-BEYOND): a double-blind, randomised controlled phase 3 trial

(2018) Mark C Genovese et al.   LANCET

Safety and efficacy of upadacitinib in patients with rheumatoid arthritis and inadequate response to conventional synthetic disease-modifying anti-rheumatic drugs (SELECT-NEXT): a randomised, double-blind, placebo-controlled phase 3 trial

(2018) Gerd R Burmester et al.   LANCET

Kinase inhibitors: the road ahead

(2018) Fleur M. Ferguson et al.   NATURE REVIEWS DRUG DISCOVERY

Genetic predictors of efficacy and toxicity of iguratimod in patients with rheumatoid arthritis

(2018) Wenjing Xiao et al.   PHARMACOGENOMICS

Response to baricitinib based on prior biologic use in patients with refractory rheumatoid arthritis

(2018) Mark C Genovese et al.   RHEUMATOLOGY

A pooled analysis of the safety of tofacitinib as monotherapy or in combination with background conventional synthetic disease-modifying antirheumatic drugs in a Phase 3 rheumatoid arthritis population

(2018) Alan J. Kivitz et al.   SEMINARS IN ARTHRITIS AND RHEUMATISM

Impact of Sustained Remission on the Risk of Serious Infection in Patients With Rheumatoid Arthritis

(2018) Neil A. Accortt et al.   ARTHRITIS CARE & RESEARCH

T-614 Promotes Osteoblastic Cell Differentiation by Increasing Dlx5 Expression and Regulating the Activation of p38 and NF-κB

(2018) Jinglue Song et al.   Biomed Research International

Suspected drug-induced liver injury associated with iguratimod: a case report and review of the literature

(2018) Xiao-li Li et al.   BMC GASTROENTEROLOGY

Safety Profile of Baricitinib in Patients with Active Rheumatoid Arthritis with over 2 Years Median Time in Treatment

(2018) Josef S. Smolen et al.   JOURNAL OF RHEUMATOLOGY

OUP accepted manuscript

(2018)   RHEUMATOLOGY

Comparative Price Analysis of Biological Products for Treatment of Rheumatoid Arthritis

(2018) Manoela Manova et al.   Frontiers in Pharmacology

Comparative risk of venous thromboembolism with tofacitinib versus tumor necrosis factor inhibitors: A cohort study of rheumatoid arthritis patients

(2018) Rishi J. Desai et al.   Arthritis & Rheumatology

Anticancer kinase inhibitors impair intracellular viral trafficking and exert broad-spectrum antiviral effects

(2017) Elena Bekerman et al.   JOURNAL OF CLINICAL INVESTIGATION

Efficacy and safety of tofacitinib monotherapy, tofacitinib with methotrexate, and adalimumab with methotrexate in patients with rheumatoid arthritis (ORAL Strategy): a phase 3b/4, double-blind, head-to-head, randomised controlled trial

(2017) Roy Fleischmann et al.   LANCET

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

Tofacitinib improves atherosclerosis despite up-regulating serum cholesterol in patients with active rheumatoid arthritis: a cohort study

(2017) Kensuke Kume et al.   RHEUMATOLOGY INTERNATIONAL

Peficitinib, a JAK Inhibitor, in the Treatment of Moderate-to-Severe Rheumatoid Arthritis in Patients With an Inadequate Response to Methotrexate

(2017) A. J. Kivitz et al.   Arthritis & Rheumatology

Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK-1 Inhibitor, After Short-Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials

(2017) Frédéric Vanhoutte et al.   Arthritis & Rheumatology

Peficitinib, a JAK Inhibitor, in Combination With Limited Conventional Synthetic Disease-Modifying Antirheumatic Drugs in the Treatment of Moderate-to-Severe Rheumatoid Arthritis

(2017) Mark C. Genovese et al.   Arthritis & Rheumatology

Anifrolumab, an Anti-Interferon-α Receptor Monoclonal Antibody, in Moderate-to-Severe Systemic Lupus Erythematosus

(2017) Richard Furie et al.   Arthritis & Rheumatology

Baricitinib, Methotrexate, or Combination in Patients With Rheumatoid Arthritis and No or Limited Prior Disease-Modifying Antirheumatic Drug Treatment

(2017) Roy Fleischmann et al.   Arthritis & Rheumatology

The EULAR points to consider for use of antirheumatic drugs before pregnancy, and during pregnancy and lactation

(2016) Carina Götestam Skorpen et al.   ANNALS OF THE RHEUMATIC DISEASES

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

Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis

(2016) Shingo Nakayamada et al.   BIODRUGS

SARS coronavirus papain-like protease induces Egr-1-dependent up-regulation of TGF-β1 via ROS/p38 MAPK/STAT3 pathway

(2016) Shih-Wein Li et al.   Scientific Reports

Efficacy and Safety of ABT-494, a Selective JAK-1 Inhibitor, in a Phase IIb Study in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate

(2016) Mark C. Genovese et al.   Arthritis & Rheumatology

A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy

(2016) Joel M. Kremer et al.   Arthritis & Rheumatology

Efficacy and safety of tofacitinib following inadequate response to conventional synthetic or biological disease-modifying antirheumatic drugs

(2015) Christina Charles-Schoeman et al.   ANNALS OF THE RHEUMATIC DISEASES

Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study

(2015) Tsutomu Takeuchi et al.   ANNALS OF THE RHEUMATIC DISEASES

The role of BAFF in the progression of rheumatoid arthritis

(2015) Fang Wei et al.   CYTOKINE

Regulatory Effect of Iguratimod on the Balance of Th Subsets and Inhibition of Inflammatory Cytokines in Patients with Rheumatoid Arthritis

(2015) Yunzhi Xu et al.   MEDIATORS OF INFLAMMATION

IL-12 and IL-23 cytokines: from discovery to targeted therapies for immune-mediated inflammatory diseases

(2015) Michele W L Teng et al.   NATURE MEDICINE

Type I/II cytokines, JAKs and new strategies for treating autoimmune diseases

(2015) Daniella M. Schwartz et al.   Nature Reviews Rheumatology

Potential Mechanisms Leading to the Abnormal Lipid Profile in Patients With Rheumatoid Arthritis Versus Healthy Volunteers and Reversal by Tofacitinib

(2015) Christina Charles-Schoeman et al.   Arthritis & Rheumatology

2015 American College of Rheumatology Guideline for the Treatment of Rheumatoid Arthritis

(2015) Jasvinder A. Singh et al.   Arthritis & Rheumatology

Genetic studies reveal an unexpected negative regulatory role for Jak2 in thrombopoiesis

(2014) S. C. Meyer et al.   BLOOD

Concomitant iguratimod therapy in patients with active rheumatoid arthritis despite stable doses of methotrexate: a randomized, double-blind, placebo-controlled trial

(2014) Naoki Ishiguro et al.   Modern Rheumatology

Tofacitinib versus Methotrexate in Rheumatoid Arthritis

(2014) Eun Bong Lee et al.   NEW ENGLAND JOURNAL OF MEDICINE

The activity of JAK-STAT pathways in rheumatoid arthritis: constitutive activation of STAT3 correlates with interleukin 6 levels

(2014) Pia Isomäki et al.   RHEUMATOLOGY

Activation of Syk in Peripheral Blood B Cells in Patients With Rheumatoid Arthritis: A Potential Target for Abatacept Therapy

(2014) Shigeru Iwata et al.   Arthritis & Rheumatology

Tofacitinib in Combination With Nonbiologic Disease-Modifying Antirheumatic Drugs in Patients With Active Rheumatoid Arthritis

(2013) Joel Kremer et al.   ANNALS OF INTERNAL MEDICINE

Tofacitinib (CP-690,550) in patients with rheumatoid arthritis receiving methotrexate: Twelve-month data from a twenty-four-month phase III randomized radiographic study

(2013) Désirée van der Heijde et al.   ARTHRITIS AND RHEUMATISM

Longterm Safety and Efficacy of Tocilizumab in Patients with Rheumatoid Arthritis: A Cumulative Analysis of Up to 4.6 Years of Exposure

(2013) M. C. Genovese et al.   JOURNAL OF RHEUMATOLOGY

Tofacitinib (CP-690,550) in combination with methotrexate in patients with active rheumatoid arthritis with an inadequate response to tumour necrosis factor inhibitors: a randomised phase 3 trial

(2013) Gerd R Burmester et al.   LANCET

Safety and efficacy of combination therapy of iguratimod with methotrexate for patients with active rheumatoid arthritis with an inadequate response to methotrexate: An open-label extension of a randomized, double-blind, placebo-controlled trial

(2013) Masako Hara et al.   Modern Rheumatology

Targeting the SYK–BTK axis for the treatment of immunological and hematological disorders

(2013) Seng-Lai Tan et al.   PHARMACOLOGY & THERAPEUTICS

Risk of Venous Thromboembolism in Patients With Rheumatoid Arthritis and Association With Disease Duration and Hospitalization

(2012) Marie E. Holmqvist et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis

(2012) Roy Fleischmann et al.   NEW ENGLAND JOURNAL OF MEDICINE

Tyr323-dependent p38 activation is associated with rheumatoid arthritis and correlates with disease activity

(2011) Mercedes López-Santalla et al.   ARTHRITIS AND RHEUMATISM

Interferon signals and monocytic sensitization of the interferon-γ signaling pathway in the peripheral blood of patients with rheumatoid arthritis

(2011) Thomas Karonitsch et al.   ARTHRITIS AND RHEUMATISM

The lifetime risk of adult-onset rheumatoid arthritis and other inflammatory autoimmune rheumatic diseases

(2010) Cynthia S. Crowson et al.   ARTHRITIS AND RHEUMATISM

Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis

(2009) Stanley B. Cohen et al.   ARTHRITIS AND RHEUMATISM

Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: Results of two randomized, double-blind, placebo-controlled clinical studies

(2009) Nemanja Damjanov et al.   ARTHRITIS AND RHEUMATISM

Inhibition of p38: Has the fat lady sung?

(2009) Mark C. Genovese   ARTHRITIS AND RHEUMATISM

The p38α Kinase Plays a Central Role In Inflammation

(2009) Gary Schieven   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Intracellular signal pathways: Potential for therapies

(2009) Melissa Mavers et al.   Current Rheumatology Reports

Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity

(2008) R. J. Hill et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS