Abstract Number: 1587 • 2016 ACR/ARHP Annual Meeting
A Phase 2a, 4-Week Double-Blind, Proof-of-Concept Efficacy and Safety Study of CC-292 Versus Placebo As Co-Therapy with Methotrexate in Active Rheumatoid Arthritis (RA)
Methods: 47 adult female RA subjects were randomized 1:1 CC-292 375 mg PO daily or placebo (PBO). Subjects were required to have a diagnosis of…Abstract Number: 1642 • 2016 ACR/ARHP Annual Meeting
Pharmacokinetic-Pharmacodynamic Analysis of GS-4059-Mediated Bruton’s Tyrosine Kinase Inhibition
Background/Purpose: GS-4059 is a covalent inhibitor of Bruton’s Tyrosine Kinase (BTK) under development for the treatment of rheumatoid arthritis (RA) and oncology. This work aimed…Abstract Number: 2109 • 2016 ACR/ARHP Annual Meeting
Immunoprofiling of Bruton’s Tyrosine Kinase (Btk)/Tec Family Kinase Inhibitors Indicate Activities Beyond Btk in Immunocyte Function
Background/Purpose: CC-292, CC-90008, and ibrutinib are covalent Btk/Tec family kinase inhibitors that block Btk activity by binding with high affinity to the adenosine triphosphate (ATP)…Abstract Number: 2622 • 2016 ACR/ARHP Annual Meeting
Safety, Pharmacokinetics, and Biomarker Profile from Phase 1 Clinical Trials of Healthy Volunteers Treated with GDC-0853, a Highly Selective Reversible Oral Bruton’s Tyrosine Kinase (BTK) Inhibitor
Background/Purpose: B cell depletion therapy has provided evidence of the importance of B cells in the pathogenesis of rheumatoid arthritis and other inflammatory diseases. Consequently,…Abstract Number: 2785 • 2016 ACR/ARHP Annual Meeting
Translatable in Vitro Immunocyte Functional Measures of CC-292 and CC-90008 Inhibitors of the Bruton’s Tyrosine Kinase (Btk)/Tec Family and the Pathology Observed in the MLR/Lpr Mouse Model of Systemic Lupus Erythematosus (SLE)
Background/Purpose: CC-292 and CC-90008 are covalent Btk/Tec family kinase inhibitors that block Btk activity by binding with high affinity to the adenosine triphosphate (ATP) binding…Abstract Number: 1771 • 2015 ACR/ARHP Annual Meeting
Blockade of Immune Complex-Mediated Glomerulonephritis By Highly Selective Inhibition of Bruton’s Tyrosine Kinase
Background/Purpose: Renal disease with loss of organ function results in significant morbidity and mortality in SLE. In the kidneys of affected patients, autoantibody-containing immune complexes…Abstract Number: 2561 • 2015 ACR/ARHP Annual Meeting
TAS5315, a Novel Bruton’s Tyrosine Kinase (BTK) Inhibitor, Demonstrates Potent Efficacy in an Animal Model of Rheumatoid Arthritis
Background/Purpose: Bruton’s tyrosine kinase (BTK) is a member of the Tec family kinases, and is expressed in B cells, monocytes/macrophages, mast cells, basophils and osteoclast1,2.…Abstract Number: 1093 • 2015 ACR/ARHP Annual Meeting
Activation of Syk-Btk Signal in Peripheral Blood B Cells in Patients with Rheumatoid Arthritis: A Potential Target for Abatacept Therapy
Background/Purpose: B cells play a pivotal role in the pathogenesis of autoimmune diseases. Although Syk function as a key molecule in BCR signaling, the pathological…Abstract Number: 1106 • 2015 ACR/ARHP Annual Meeting
Efficacy of Abbv-105, a Selective and Irreversible Inhibitor of Bruton’s Tyrosine Kinase (BTK), in Multiple Models of Inflammation
Background/Purpose: Bruton’s Tyrosine Kinase (BTK) is a non-receptor tyrosine kinase required for intracellular signaling pathways downstream of several key immunoreceptors, including the B cell receptor,…Abstract Number: 1124 • 2015 ACR/ARHP Annual Meeting
Bruton’s Tyrosine Kinase Levels Are Increased in B Cells from Patients with Primary Sjögren’s Syndrome
Background/Purpose: Upon B cell receptor stimulation, B cells increase protein expression levels of the key downstream signaling molecule Bruton’s tyrosine kinase (BTK). BTK-transgenic mice that…Abstract Number: 1671 • 2015 ACR/ARHP Annual Meeting
Discovery of PRN1008, a Novel, Reversible Covalent BTK Inhibitor in Clinical Development for Rheumatoid Arthritis
Background/Purpose: There is strong pre-clinical validation for Bruton’s Tyrosine Kinase (BTK) as a therapeutic target for autoimmune diseases based on multiple animal models. Principia discovered…Abstract Number: 1209 • 2014 ACR/ARHP Annual Meeting
Anti-Scavenger Receptor Autoantibodies Disrupted Marginal Zone Macrophage Integrity Via Bruton’s Tyrosine Kinase
Background/Purpose Ibrutinib, a Btk kinase activity inhibitor, is a novel inhibitor under development for autoimmune disease therapy. We have shown that Btk was significantly upregulated…Abstract Number: 646 • 2014 ACR/ARHP Annual Meeting
ONO-4059 – a Highly Potent and Dual Oral Inhibitor of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase: Improves Anti-Nuclear Antibodies–mediated SLE in Mice
Background/Purpose: Systemic Lupus Erythematosus (SLE) is a complex and heterogeneous autoimmune disease associated with the over production of high affinity autoantibodies, mainly raised against nuclear…Abstract Number: 2353 • 2013 ACR/ARHP Annual Meeting
Evaluation Of An Irreversible Dual Target Inhibitor (AC0025) Of Bruton’s Tryosine Kinase and Janus Kinase 3 As a Therapeutic Agent For Rheumatoid Arthritis
Background/Purpose: Bruton’s Tryosine Kinase (BTK) and Janus Kinase 3 (JAK3) are intimately involved in the signaling pathways regulating B cell and T cell functions. Perturbing…Abstract Number: 1824 • 2013 ACR/ARHP Annual Meeting
ONO-4059 – A Novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase- Suppresses Osteoclastic Bone Resorption and Inflammation
Background/Purpose: Rheumatoid arthritis (RA) is a systemic autoimmune disease characterized by leukocyte infiltration, synoviocyte hyperplasia and osteoclastogenesis, leading to erosion of the joints and cartilage,…
ACR Meeting Abstracts