|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Pharmacokinetic/pharmacodynamic modeling showed that mean BTK occupancy in blood cells of 80% was linked to near-complete disease inhibition in both RA and SLE mouse models.
|
30988116 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
BTK protein levels were significantly increased in transitional and naïve B cells of active GPA and RA patients compared with remission GPA patients and HCs.
|
31209475 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Bruton's tyrosine kinase (BTK) in macrophages and B cells has been demonstrated to be a promising therapeutic target for RA.
|
31495833 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.
|
30875504 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
As a result, pharmacological inhibition of BTK is anticipated to provide an effective strategy for the clinical treatment of autoimmune diseases such as rheumatoid arthritis and lupus.
|
30893553 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Bruton's tyrosine kinase (BTK) is a known drug target for B cell malignancies and autoimmune diseases like rheumatoid arthritis.
|
31172362 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.
|
31260299 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
This strategy has been successfully applied to the measurement of the RO for Bruton's tyrosine kinase (BTK) in the blood lysate of monkeys after dosing with branebrutinib (BMS-986195), a covalent BTK inhibitor being evaluated to treat rheumatoid arthritis.
|
31247719 |
2019 |
|
Rheumatoid Arthritis
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Preclinical studies have indicated that inhibition of Btk activity might offer a potential therapy in autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus.
|
29457982 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
GeneticVariation
|
disease |
BEFREE |
Because of this overwhelming evidence of a pathogenic role of BTK in autoimmunity, several clinical trials in rheumatoid arthritis and systemic lupus erythematosus patients with BTK inhibitors are currently running.
|
29717662 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
BTK is a promising target for the treatment of multiple diseases such as B cell malignances, asthma, and rheumatoid arthritis.
|
29198867 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheumatoid arthritis (RA).
|
29324347 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
|
30216722 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Development of Bruton's Tyrosine Kinase Inhibitors for Rheumatoid Arthritis.
|
29546831 |
2018 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
GDC-0853 ((S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one) is a selective and reversible oral small-molecule BTK inhibitor in development for the treatment of rheumatoid arthritis and systemic lupus erythematosus.
|
27821712 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
The high specificity of CHMFL-BTK-11 makes it a useful pharmacological tool to further detect BTK mediated signaling in the pathology of RA.
|
28352114 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK currently being investigated in clinical trials for the treatment of both RA and primary Sjögren's syndrome.
|
28742141 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
|
28279528 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Importantly, BTK protein and phospho-BTK were significantly increased in B cells from anti-citrullinated protein antibody (ACPA)-positive RA patients but not in B cells from ACPA-negative RA patients.
|
28141917 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
|
28720503 |
2017 |
|
Rheumatoid Arthritis
|
0.100 |
Biomarker
|
disease |
BEFREE |
Since promising effects of BTK inhibition were also seen in experimental animal models for lupus and rheumatoid arthritis, BTK may be a good target for controlling autoreactive B cells in patients with systemic autoimmune disease.
|
26341110 |
2016 |
|
Rheumatoid Arthritis
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Here, we examined the potential contributions of synovial Btk expression and activation to inflammation in rheumatoid arthritis (RA).
|
24764451 |
2015 |
|
Rheumatoid Arthritis
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Moreover, we also demonstrated that miR-346 indirectly regulated IL-18 release by indirectly inhibiting LPS-induced Bruton's tyrosine kinase expression in LPS-activated RA FLS.
|
19342689 |
2009 |