Abstract Number: 974 • 2019 ACR/ARP Annual Meeting
Bruton’s Tyrosine Kinase (BTK) Inhibitors and Autoimmune Disease: Making Sense of BTK Inhibitor Specificity Profiles and Recent Clinical Trial Successes and Failures
Background/Purpose: Clinical development of BTK/Tec family kinase inhibitors for treating autoimmune diseases has lagged that of their successful application in oncology. The lack of selective…Abstract Number: 2413 • 2019 ACR/ARP Annual Meeting
LOU064: A Highly Selective and Potent Covalent Oral BTK Inhibitor with Promising Pharmacodynamic Efficacy on B Cells for Sjoegren’s Syndrome
Background/Purpose: Bruton’s Tyrosine Kinase (BTK) is a cytoplasmic tyrosine kinase selectively expressed in B cells, macrophages, mast cells and basophils. The essential role of BTK…Abstract Number: 929 • 2019 ACR/ARP Annual Meeting
Efficacy and Safety of Fenebrutinib, a BTK Inhibitor, Compared to Placebo in Rheumatoid Arthritis Patients with Active Disease Despite TNF Inhibitor Treatment: Randomized, Double Blind, Phase 2 Study
Background/Purpose: Fenebrutinib (GDC-0853, FEN) is an orally administered, highly selective, non-covalent, and reversible small molecule inhibitor of Bruton’s Tyrosine Kinase (BTK).1 We report the efficacy…Abstract Number: 965 • 2019 ACR/ARP Annual Meeting
Discovery of DWP212525, a Potent JAK3 and BTK Dual Target Inhibitor for the Treatment of Autoimmune Diseases
Background/Purpose: Janus Kinase (JAK) and Bruton's tyrosine kinase (BTK) play critical roles in activation and function of T cells and B cells. Dysregulation of this…Abstract Number: 967 • 2019 ACR/ARP Annual Meeting
Bruton’s Tyrosine Kinase (BTK) Pathway Is Active in Synovium at Various Stages of Rheumatoid Arthritis Disease Progression
Background/Purpose: Bruton’s tyrosine kinase (BTK), a TEC family non-receptor kinase, is expressed in B cells and myeloid cells. BTK relays signaling downstream of B cell…Abstract Number: 41 • 2018 ACR/ARHP Annual Meeting
TAS5315, a Novel Bruton’s Tyrosine Kinase Inhibitor, Improves Bone Strength in Mouse Model for Rheumatoid Arthritis
Background/Purpose: The erosions of bone and cartilage are a cardinal feature of rheumatoid arthritis (RA) and associated with disease severity and poor functional outcome. Although…Abstract Number: 1010 • 2018 ACR/ARHP Annual Meeting
Inhibition of Bruton’s Tyrosine Kinase (BTK) Prevents Inflammatory Macrophage Differentiation: A Potential Role in RA and SLE
Background/Purpose: Bruton’s Tyrosine Kinase (BTK) mediates B cell receptor (BCR) and Fc receptor (FcR) signalling in several hematopoietic cell lineages, including B cells, macrophages and…Abstract Number: 2099 • 2018 ACR/ARHP Annual Meeting
Bruton’s Tyrosine Kinase (BTK) Inhibition Modulates Multiple Cell Types Instrumental in the Pathogenesis of Lupus Nephritis
Background/Purpose: Lupus nephritis (LN) is a serious manifestation of systemic lupus erythematosus (SLE) that adds substantial morbidity and mortality. Passive transfer of pre-formed nephritogenic antibodies…Abstract Number: 29 • 2017 ACR/ARHP Annual Meeting
BTK Inhibition Ameliorates Lupus-Associated Neuropsychiatric and Skin Disease
Background/Purpose: The importance of macrophages in the pathogenesis of cutaneous and neuropsychiatric systemic lupus erythematosus (SLE) is well established. Additionally, autoantibodies produced by autoreactive…Abstract Number: 503 • 2017 ACR/ARHP Annual Meeting
BMS-986195 Is a Highly Selective and Rapidly Acting Covalent Inhibitor of Bruton’s Tyrosine Kinase with Robust Efficacy at Low Doses in Preclinical Models of RA and Lupus Nephritis
Background/Purpose: BMS-986195 is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), a member of the Tec family of non-receptor tyrosine kinases essential in…Abstract Number: 1320 • 2017 ACR/ARHP Annual Meeting
TAS5315, a Novel Bruton’s Tyrosine Kinase Inhibitor, Ameliorates Inflammation and Bone Erosion in Murine Model for Rheumatoid Arthritis
Background/Purpose: The erosions of bone and cartilage are a cardinal feature of rheumatoid arthritis (RA) and associated with disease severity and poor functional outcome. Although…Abstract Number: 2561 • 2017 ACR/ARHP Annual Meeting
BTK Inhibition Ameliorates Renal Disease in Spontaneous Murine Lupus Nephritis
Background/Purpose: Bruton's tyrosine kinase (BTK) plays an important role in B cell and FcR mediated myeloid cell activation. We recently described a selective BTK inhibitor,…Abstract Number: 2565 • 2017 ACR/ARHP Annual Meeting
Pharmacodynamic Modeling of BTK Occupancy Versus Efficacy in Ra and SLE Models Using the Novel Specific BTK Inhibitor Evobrutinib
Background/Purpose: Bruton’s tyrosine kinase (BTK) is a clinically-proven target in several hematological indications. Due to its role in mediating the signaling of both B cell…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…
ACR Meeting Abstracts