Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases

A Phase 1b, Randomized, Single-Center Trial of Topical Cerdulatinib (DMVT-502) in Patients with Mild-to-Moderate Atopic Dermatitis

(2021) Stephen C. Piscitelli et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Entospletinib and obinutuzumab in patients with relapsed/refractory chronic lymphocytic leukemia and B-cell malignancies

(2021) Adam S. Kittai et al.   HAEMATOLOGICA

Gain-of-function variants in SYK cause immune dysregulation and systemic inflammation in humans and mice

(2021) Lin Wang et al.   NATURE GENETICS

Spleen Tyrosine Kinase Inhibition Ameliorates Tubular Inflammation in IgA Nephropathy

(2021) Wai Han Yiu et al.   Frontiers in Physiology

Constitutive JAK/STAT signaling is the primary mechanism of resistance to JAKi in TYK2-rearranged acute lymphoblastic leukemia

(2021) Paniz Tavakoli Shirazi et al.   CANCER LETTERS

Spleen tyrosine kinase regulates crosstalk of hypoxia-inducible factor-1α and nuclear factor (erythroid-derived2)-like 2 for B cell survival

(2021) Ju-Won Jang et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

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

Spleen tyrosine kinase inhibition is an effective treatment for established vasculitis in a pre-clinical model

(2020) Stephen P. McAdoo et al.   KIDNEY INTERNATIONAL

Macrophage Syk–PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk–PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression

(2020) Shweta Joshi et al.   MOLECULAR CANCER THERAPEUTICS

Piceatannol: A natural stilbene for the prevention and treatment of cancer

(2020) Kishore Banik et al.   PHARMACOLOGICAL RESEARCH

Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases

(2020) Peter Blomgren et al.   ACS Medicinal Chemistry Letters

Phase Ib Study of Tirabrutinib in Combination with Idelalisib or Entospletinib in Previously Treated Chronic Lymphocytic Leukemia

(2020) Alexey V. Danilov et al.   CLINICAL CANCER RESEARCH

Pulmonary adverse events of small molecule JAK inhibitors in autoimmune disease: systematic review and meta-analysis

(2020) Jun K Khoo et al.   RHEUMATOLOGY

Kinase inhibition in autoimmunity and inflammation

(2020) Ali A. Zarrin et al.   NATURE REVIEWS DRUG DISCOVERY

Phase 1b study of tirabrutinib in combination with idelalisib or entospletinib in previously treated B-cell lymphoma

(2020) Franck Morschhauser et al.   LEUKEMIA

Safety and efficacy of fostamatinib in rheumatoid arthritis patients with an inadequate response to methotrexate in phase II OSKIRA-ASIA-1 and OSKIRA-ASIA-1X study

(2020) Yoshiya Tanaka et al.   RHEUMATOLOGY

Efficacy and Safety of Multiple Dosages of Fostamatinib in Adult Patients With Rheumatoid Arthritis: A Systematic Review and Meta-Analysis

(2019) Yaqi Kang et al.   Frontiers in Pharmacology

Design and optimization of orally spleen tyrosine kinase (SYK) inhibitors for treatment of solid tumor

(2019) Cheng Wang et al.   BIOORGANIC CHEMISTRY

Fostamatinib for the treatment of adult persistent and chronic immune thrombocytopenia: Results of two phase 3, randomized, placebo-controlled trials

(2018) James Bussel et al.   AMERICAN JOURNAL OF HEMATOLOGY

Fostamatinib: First Global Approval

(2018) Anthony Markham   DRUGS

Fostamatinib for persistent/chronic adult immune thrombocytopenia

(2018) Adrian Newland et al.   Immunotherapy

Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis

(2018) Astrid S. Clarke et al.   THROMBOSIS RESEARCH

NF-κB activation mediates LPS- or zymosan-induced hypotension and inflammation reversed by BAY61-3606, a selective Syk inhibitor, in rat models of septic and non-septic shock

(2018) Seyhan Sahan-Firat et al.   CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY

Cerdulatinib Pharmacodynamics and Relationships to Tumor Response Following Oral Dosing in Patients with Relapsed/Refractory B-cell Malignancies

(2018) Greg P. Coffey et al.   CLINICAL CANCER RESEARCH

PMA inhibits endothelial cell migration through activating the PKC-δ/Syk/NF-κB-mediated up-regulation of Thy-1

(2018) Heng-Ching Wen et al.   Scientific Reports

Inhibition of spleen tyrosine kinase attenuates psoriasis-like inflammation in mice through blockade of dendritic cell-Th17 inflammation axis

(2018) Khalid S. Alzahrani et al.   BIOMEDICINE & PHARMACOTHERAPY

Syk inhibitors in clinical development for hematological malignancies

(2017) Delong Liu et al.   Journal of Hematology & Oncology

Syk Regulates Neutrophilic Airway Hyper-Responsiveness in a Chronic Mouse Model of Allergic Airways Inflammation

(2017) Sepehr Salehi et al.   PLoS One

BAY61-3606 potentiates the anti-tumor effects of TRAIL against colon cancer through up-regulating DR4 and down-regulating NF-κB

(2016) Jipei Du et al.   CANCER LETTERS

The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia

(2016) Matthew D. Blunt et al.   CLINICAL CANCER RESEARCH

Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers

(2016) Srini Ramanathan et al.   CLINICAL DRUG INVESTIGATION

Update on Lupus Nephritis

(2016) Salem Almaani et al.   Clinical Journal of the American Society of Nephrology

PRT062607 Achieves Complete Inhibition of the Spleen Tyrosine Kinase at Tolerated Exposures Following Oral Dosing in Healthy Volunteers

(2016) Greg Coffey et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells

(2016) Catherine M. K. Ho et al.   PLoS One

Fostamatinib, an oral spleen tyrosine kinase inhibitor, in the treatment of rheumatoid arthritis: a meta-analysis of randomized controlled trials

(2016) Sumit Kunwar et al.   RHEUMATOLOGY INTERNATIONAL

Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors

(2015) Jang-Sik Choi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia

(2015) J. Sharman et al.   BLOOD

The Syk Inhibitor Fostamatinib Decreases the Severity of Colonic Mucosal Damage in a Rodent Model of Colitis

(2015) Guray Can et al.   Journal of Crohns & Colitis

Human autoimmune diseases: a comprehensive update

(2015) Lifeng Wang et al.   JOURNAL OF INTERNAL MEDICINE

Selective spleen tyrosine kinase inhibition delays autoimmune arthritis in mice

(2015) ZUOFU ZHANG et al.   Molecular Medicine Reports

Simultaneous inhibition of JAK and SYK kinases ameliorates chronic and destructive arthritis in mice

(2015) Alba Llop-Guevara et al.   ARTHRITIS RESEARCH & THERAPY

Pharmacokinetic-pharmacodynamic modeling of fostamatinib efficacy on ACR20 to support dose selection in patients with rheumatoid arthritis (RA)

(2014) John Maringwa et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase

(2014) Kevin S. Currie et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Phase III, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Study of 2 Dosing Regimens of Fostamatinib in Patients with Rheumatoid Arthritis with an Inadequate Response to a Tumor Necrosis Factor-  Antagonist

(2014) M. C. Genovese et al.   JOURNAL OF RHEUMATOLOGY

Increased Syk phosphorylation leads to overexpression of TRAF6 in peripheral B cells of patients with systemic lupus erythematosus

(2014) S Iwata et al.   LUPUS

Therapeutic Potential of Spleen Tyrosine Kinase Inhibition for Treating High-Risk Precursor B Cell Acute Lymphoblastic Leukemia

(2014) T. Perova et al.   Science Translational Medicine

Getting Syk: spleen tyrosine kinase as a therapeutic target

(2014) Robert L. Geahlen   TRENDS IN PHARMACOLOGICAL SCIENCES

Effects of Fostamatinib, an Oral Spleen Tyrosine Kinase Inhibitor, in Rheumatoid Arthritis Patients With an Inadequate Response to Methotrexate: Results From a Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study

(2014) Michael E. Weinblatt et al.   Arthritis & Rheumatology

Safety profile of protein kinase inhibitors in rheumatoid arthritis: systematic review and meta-analysis

(2013) Eva Salgado et al.   ANNALS OF THE RHEUMATIC DISEASES

Inhibition of spleen tyrosine kinase in the treatment of rheumatoid arthritis

(2013) J. S. Nijjar et al.   RHEUMATOLOGY

Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: implications for SYK inhibitors in autoimmune disease therapy

(2013) Cheng Liao et al.   ARTHRITIS RESEARCH & THERAPY

Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

(2012) Tadeusz Robak et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Inhibition of spleen tyrosine kinase as treatment of postoperative ileus

(2012) Sjoerd H W van Bree et al.   GUT

Spleen Tyrosine Kinase Is Important in the Production of Proinflammatory Cytokines and Cell Proliferation in Human Mesangial Cells following Stimulation with IgA1 Isolated from IgA Nephropathy Patients

(2012) M. J. Kim et al.   JOURNAL OF IMMUNOLOGY

Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration

(2012) J Hoellenriegel et al.   LEUKEMIA

Role of Spleen Tyrosine Kinase Inhibitors in the Management of Rheumatoid Arthritis

(2011) David L. Scott   DRUGS

An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis: A three-month randomized, placebo-controlled, phase II study in patients with active rheumatoid arthritis that did not respond to biologic agents

(2010) Mark C. Genovese et al.   ARTHRITIS AND RHEUMATISM

The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the E - TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling

(2010) M. Suljagic et al.   BLOOD

Spleen tyrosine kinases: biology, therapeutic targets and drugs

(2010) Mauro Riccaboni et al.   DRUG DISCOVERY TODAY

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

(2010) R. Eric Davis et al.   NATURE

An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis

(2010) Michael E. Weinblatt et al.   NEW ENGLAND JOURNAL OF MEDICINE

Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey

(2010) D. J. Sweeny et al.   XENOBIOTICA

Structural Insights for Design of Potent Spleen Tyrosine Kinase Inhibitors from Crystallographic Analysis of Three Inhibitor Complexes

(2009) Armando G. Villaseñor et al.   Chemical Biology & Drug Design

Syk kinase inhibitors in allergic diseases

(2009) J. Denyer et al.   DRUG NEWS & PERSPECTIVES

A novel Syk kinase inhibitor suitable for inhalation: R-343(?) – WO-2009031011

(2009) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Treatment of rheumatoid arthritis with a syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial

(2008) Michael E. Weinblatt et al.   ARTHRITIS AND RHEUMATISM

An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus

(2008) Frances Rena Bahjat et al.   ARTHRITIS AND RHEUMATISM