Investigational Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis

Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability

(2016) Wendy B. Young et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SP0100 Axial Spa: What is the Effect of Gender, Age and Disease Duration on Treatment Efficacy?

(2015) I.E. van der Horst-Bruinsma   ANNALS OF THE RHEUMATIC DISEASES

OP0026-PARE Campaign for Early and Accurate Diagnosis and Early Intervention in RMDS

(2015) A. Stara   ANNALS OF THE RHEUMATIC DISEASES

Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834

(2015) Wendy B. Young et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton’s Tyrosine Kinase (BTK) inhibitor scaffold

(2015) Yan Lou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Abstract 2596: ACP-196: a novel covalent Bruton's tyrosine kinase (Btk) inhibitor with improved selectivity and in vivo target coverage in chronic lymphocytic leukemia (CLL) patients

(2015) Todd Covey et al.   CANCER RESEARCH

Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase

(2015) Christopher R. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prolonged and tunable residence time using reversible covalent kinase inhibitors

(2015) J Michael Bradshaw et al.   Nature Chemical Biology

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

(2015) Jian Liu et al.   ACS Medicinal Chemistry Letters

THU0499 Hm71224, A Novel Oral BTK Inhibitor, Inhibits Human Immune Cell Activation: New Drug Candidate to Treat B-Cell Associated Autoimmune Diseases

(2014) J.K. Park et al.   ANNALS OF THE RHEUMATIC DISEASES

Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases

(2014) Qing Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis

(2014) Jennifer A. Whang et al.   DRUG DISCOVERY TODAY

Structure-Based Drug Design of RN486, a Potent and Selective Bruton’s Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis

(2014) Yan Lou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Clinical Targeting of Mutated and Wild-Type Protein Tyrosine Kinases in Cancer

(2014) J. M. Drake et al.   MOLECULAR AND CELLULAR BIOLOGY

Cell-Cycle Reprogramming for PI3K Inhibition Overrides a Relapse-Specific C481S BTK Mutation Revealed by Longitudinal Functional Genomics in Mantle Cell Lymphoma

(2014) D. Chiron et al.   Cancer Discovery

The orally available Btk inhibitor ibrutinib (PCI-32765) protects against osteoclast-mediated bone loss

(2013) Masahiro Shinohara et al.   BONE

B-Cell Receptor Signaling Inhibitors for Treatment of Autoimmune Inflammatory Diseases and B-Cell Malignancies

(2013) Kamal D. Puri et al.   INTERNATIONAL REVIEWS OF IMMUNOLOGY

Kinase inhibitors: a new class of antirheumatic drugs

(2012) Vasileios Kyttaris   Drug Design Development and Therapy

Targeting lymphocyte signaling pathways as a therapeutic approach to systemic lupus erythematosus

(2011) Vasileios C. Kyttaris et al.   CURRENT OPINION IN RHEUMATOLOGY

Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor

(2011) L. Liu et al.   DRUG METABOLISM AND DISPOSITION

TEC family kinases in health and disease - loss-of-function of BTK and ITK and the gain-of-function fusions ITK-SYK and BTK-SYK

(2011) Alamdar Hussain et al.   FEBS Journal

Antiarthritis Effect of a Novel Bruton's Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and Efficacy

(2011) L. Liu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Kinase inhibitors: a new approach to rheumatoid arthritis treatment

(2010) Stanley Cohen et al.   CURRENT OPINION IN RHEUMATOLOGY

Specific Btk inhibition suppresses B cell– and myeloid cell–mediated arthritis

(2010) Julie A Di Paolo et al.   Nature Chemical Biology

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Tec kinases regulate T-lymphocyte development and function: new insights into the roles of Itk and Rlk/Txk

(2009) Julie A. Readinger et al.   IMMUNOLOGICAL REVIEWS

Rituximab therapy reduces activated B cells in both the peripheral blood and bone marrow of patients with rheumatoid arthritis: depletion of memory B cells correlates with clinical response

(2009) Magda Nakou et al.   ARTHRITIS RESEARCH & THERAPY