Bruton tyrosine kinase inhibitors for multiple sclerosis

Central nervous system macrophages in progressive multiple sclerosis: relationship to neurodegeneration and therapeutics

(2022) Emily Kamma et al.   Journal of Neuroinflammation

The role of glial cells in multiple sclerosis disease progression

(2022) Luke M. Healy et al.   Nature Reviews Neurology

Slowly Expanding Lesions Predict 9-Year Multiple Sclerosis Disease Progression

(2022) Paolo Preziosa et al.   Neurology-Neuroimmunology & Neuroinflammation

BTK inhibition limits B-cell–T-cell interaction through modulation of B-cell metabolism: implications for multiple sclerosis therapy

(2022) Rui Li et al.   ACTA NEUROPATHOLOGICA

The Contribution of Neuropathology to Multiple Sclerosis Research

(2022) Hans Lassmann   EUROPEAN JOURNAL OF NEUROLOGY

All Bruton’s tyrosine kinase inhibitors have similar efficacy and risks: No

(2022) Dalia L Rotstein   Multiple Sclerosis Journal

Slowly Expanding Lesions

(2022) Sarah B. Simmons et al.   NEUROLOGY

Human T-bet+ B cell development is associated with BTK activity and suppressed by evobrutinib

(2022) Liza Rijvers et al.   JCI Insight

Facing the urgency of therapies for progressive MS — a Progressive MS Alliance proposal

(2021) Fernando Dangond et al.   Nature Reviews Neurology

Comparative Analysis of BTK Inhibitors and Mechanisms Underlying Adverse Effects

(2021) H. Yesid Estupiñán et al.   Frontiers in Cell and Developmental Biology

Imaging meningeal inflammation in CNS autoimmunity identifies a therapeutic role for BTK inhibition

(2021) Pavan Bhargava et al.   BRAIN

Remibrutinib (LOU064): A selective potent oral BTK inhibitor with promising clinical safety and pharmacodynamics in a randomized phase I trial

(2021) Martin Kaul et al.   CTS-Clinical and Translational Science

Ibrutinib combinations in CLL therapy: scientific rationale and clinical results

(2021) Natalia Timofeeva et al.   Blood Cancer Journal

Targeting Inflammasomes to Treat Neurological Diseases

(2021) Jan D. Lünemann et al.   ANNALS OF NEUROLOGY

MOG autoantibodies trigger a tightly-controlled FcR and BTK-driven microglia proliferative response

(2021) Kathryn Pellerin et al.   BRAIN

Bruton's tyrosine kinase inhibition in the treatment of preclinical models and multiple sclerosis

(2021) Anja Steinmaurer et al.   CURRENT PHARMACEUTICAL DESIGN

Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective

(2021) Chiara Brullo et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cellular immunology of relapsing multiple sclerosis: interactions, checks, and balances

(2021) Amit Bar-Or et al.   LANCET NEUROLOGY

BTK inhibitors as potential therapies for multiple sclerosis

(2021) Jorge Correale   LANCET NEUROLOGY

Safety and efficacy of tolebrutinib, an oral brain-penetrant BTK inhibitor, in relapsing multiple sclerosis: a phase 2b, randomised, double-blind, placebo-controlled trial

(2021) Daniel S Reich et al.   LANCET NEUROLOGY

Sustained reduction of serum neurofilament light chain over 7 years by alemtuzumab in early relapsing–remitting MS

(2021) Jens Kuhle et al.   Multiple Sclerosis Journal

Slowly expanding lesions are a marker of progressive MS – Yes

(2021) Martina Absinta et al.   Multiple Sclerosis Journal

A lymphocyte–microglia–astrocyte axis in chronic active multiple sclerosis

(2021) Martina Absinta et al.   NATURE

B cells in multiple sclerosis — from targeted depletion to immune reconstitution therapies

(2021) Maria T. Cencioni et al.   Nature Reviews Neurology

Concentration of evobrutinib, a BTK inhibitor, in cerebrospinal fluid during treatment of patients with relapsing multiple sclerosis in a phase 2 study

(2021) Karolina Piasecka-Stryczynska et al.   Multiple Sclerosis and Related Disorders

Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors

(2021) Rula Zain et al.   Frontiers in Immunology

Next generation antibody-based therapies in neurology

(2021) Tobias Ruck et al.   BRAIN

Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168)

(2021) Timothy D. Owens et al.   CTS-Clinical and Translational Science

Inhibition of Bruton Tyrosine Kinase Reduces Neuroimmune Cascade and Promotes Recovery after Spinal Cord Injury

(2021) Chen Guang Yu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Mechanism-based criteria to improve therapeutic outcomes in progressive multiple sclerosis

(2021) Heather Y. F. Yong et al.   Nature Reviews Neurology

Bruton’s Tyrosine Kinase (BTK) Inhibitors and Autoimmune Diseases: Making Sense of BTK Inhibitor Specificity Profiles and Recent Clinical Trial Successes and Failures

(2021) Garth E. Ringheim et al.   Frontiers in Immunology

Bruton’s Tyrosine Kinase Inhibitors: A New Generation of Promising Agents for Multiple Sclerosis Therapy

(2021) Antonio García-Merino   Cells

Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2020) Daniela Angst et al.   JOURNAL OF MEDICINAL CHEMISTRY

Adenosine-producing regulatory B cells in head and neck cancer

(2020) Sandra S. Jeske et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

A Fast and Clean BTK Inhibitor

(2020) Ronen Gabizon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Microglia in Multiple Sclerosis: Friend or Foe?

(2020) Brooke L. Guerrero et al.   Frontiers in Immunology

Inhibition of Bruton’s tyrosine kinase interferes with pathogenic B-cell development in inflammatory CNS demyelinating disease

(2020) Sebastian Torke et al.   ACTA NEUROPATHOLOGICA

A RANDOMIZED PHASE 3 TRIAL OF ZANUBRUTINIB VERSUS IBRUTINIB IN SYMPTOMATIC WALDENSTRÖM MACROGLOBULINEMIA:THE ASPEN STUDY

(2020) Constantine S. Tam et al.   BLOOD

Molecular signature of slowly expanding lesions in progressive multiple sclerosis

(2020) Katharina Jäckle et al.   BRAIN

Inhibition of Bruton´s tyrosine kinase as a novel therapeutic approach in multiple sclerosis

(2020) Sebastian Torke et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

The role of chemokines and chemokine receptors in multiple sclerosis

(2020) Li-Yuan Cui et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Predictive value of optical coherence tomography, multifocal visual evoked potentials, and full-field visual evoked potentials of the fellow, non-symptomatic eye for subsequent multiple sclerosis development in patients with acute optic neuritis

(2020) Gorm Pihl-Jensen et al.   Multiple Sclerosis Journal

Ofatumumab versus Teriflunomide in Multiple Sclerosis

(2020) Stephen L. Hauser et al.   NEW ENGLAND JOURNAL OF MEDICINE

The role of B cells in Multiple Sclerosis and related disorders

(2020) Giancarlo Comi et al.   ANNALS OF NEUROLOGY

Brain TSPO-PET predicts later disease progression independent of relapses in multiple sclerosis

(2020) Marcus Sucksdorff et al.   BRAIN

Bruton’s tyrosine kinase inhibitors: a promising emerging treatment option for multiple sclerosis

(2020) Edgar Carnero Contentti et al.   EXPERT OPINION ON EMERGING DRUGS

In vivo imaging of chronic active lesions in multiple sclerosis

(2020) Alberto Calvi et al.   Multiple Sclerosis Journal

BTK Inhibition Impairs the Innate Response Against Fungal Infection in Patients With Chronic Lymphocytic Leukemia

(2020) Stefania Fiorcari et al.   Frontiers in Immunology

B cell depletion therapies in autoimmune disease: advances and mechanistic insights

(2020) Dennis S. W. Lee et al.   NATURE REVIEWS DRUG DISCOVERY

Managing toxicities of Bruton tyrosine kinase inhibitors

(2020) Andrew Lipsky et al.   Hematology-American Society of Hematology Education Program

Understanding phosphoinositides: rare, dynamic, and essential membrane phospholipids

(2019) Eamonn J. Dickson et al.   BIOCHEMICAL JOURNAL

Pathogenic Mechanisms Associated With Different Clinical Courses of Multiple Sclerosis

(2019) Hans Lassmann   Frontiers in Immunology

Targeting Microglia and Macrophages: A Potential Treatment Strategy for Multiple Sclerosis

(2019) Jiaying Wang et al.   Frontiers in Pharmacology

Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models

(2019) Philipp Haselmayer et al.   JOURNAL OF IMMUNOLOGY

Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis

(2019) Xavier Montalban et al.   NEW ENGLAND JOURNAL OF MEDICINE

Trial of intrathecal rituximab in progressive multiple sclerosis patients with evidence of leptomeningeal contrast enhancement

(2019) Pavan Bhargava et al.   Multiple Sclerosis and Related Disorders

Impact of B cells to the pathophysiology of multiple sclerosis

(2019) Borros M. Arneth   Journal of Neuroinflammation

The pro-remyelination properties of microglia in the central nervous system

(2019) Amy F. Lloyd et al.   Nature Reviews Neurology

Imaging in mice and men: pathophysiological insights into multiple sclerosis from conventional and advanced MRI techniques

(2019) Julia Krämer et al.   PROGRESS IN NEUROBIOLOGY

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

(2019) Richard D. Caldwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Progressive multiple sclerosis: from pathophysiology to therapeutic strategies

(2019) Simon Faissner et al.   NATURE REVIEWS DRUG DISCOVERY

When encephalitogenic T cells collaborate with microglia in multiple sclerosis

(2019) Yifei Dong et al.   Nature Reviews Neurology

Central Nervous System Remyelination: Roles of Glia and Innate Immune Cells

(2019) Charbel S. Baaklini et al.   Frontiers in Molecular Neuroscience

Safety, Tolerability, Pharmacokinetics, Target Occupancy, and Concentration‐QT Analysis of the Novel BTK Inhibitor Evobrutinib in Healthy Volunteers

(2019) Andreas Becker et al.   CTS-Clinical and Translational Science

Immune reconstitution therapies: concepts for durable remission in multiple sclerosis

(2019) Jan D. Lünemann et al.   Nature Reviews Neurology

Resolution of inflammation during multiple sclerosis

(2019) F. Ruiz et al.   Seminars in Immunopathology

Progressive multiple sclerosis patients show substantial lesion activity that correlates with clinical disease severity and sex: a retrospective autopsy cohort analysis

(2018) Sabina Luchetti et al.   ACTA NEUROPATHOLOGICA

Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Volunteers Treated With GDC-0853, a Selective Reversible Bruton's Tyrosine Kinase Inhibitor

(2018) Ann E. Herman et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

The Role of Bruton's Tyrosine Kinase in Immune Cell Signaling and Systemic Autoimmunity

(2018) Jasper Rip et al.   CRITICAL REVIEWS IN IMMUNOLOGY

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review

(2018) Chengyuan Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

High-Dimensional Single-Cell Mapping of Central Nervous System Immune Cells Reveals Distinct Myeloid Subsets in Health, Aging, and Disease

(2018) Dunja Mrdjen et al.   IMMUNITY

Bruton’s Tyrosine Kinase Is Not Essential for B Cell Survival beyond Early Developmental Stages

(2018) Lindsay E. Nyhoff et al.   JOURNAL OF IMMUNOLOGY

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development

(2018) James J. Crawford et al.   JOURNAL OF MEDICINAL CHEMISTRY

Role of Bruton’s tyrosine kinase in B cells and malignancies

(2018) Simar Pal Singh et al.   Molecular Cancer

Reassessing B cell contributions in multiple sclerosis

(2018) Rui Li et al.   NATURE IMMUNOLOGY

Multiple Sclerosis: Mechanisms and Immunotherapy

(2018) Clare Baecher-Allan et al.   NEURON

Multiple Sclerosis

(2018) Daniel S. Reich et al.   NEW ENGLAND JOURNAL OF MEDICINE

Assembly mechanism of the CARMA1–BCL10–MALT1–TRAF6 signalosome

(2018) Liron David et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Slowly expanding/evolving lesions as a magnetic resonance imaging marker of chronic active multiple sclerosis lesions

(2018) Colm Elliott et al.   Multiple Sclerosis Journal

BAFF Index and CXCL13 levels in the cerebrospinal fluid associate respectively with intrathecal IgG synthesis and cortical atrophy in multiple sclerosis at clinical onset

(2017) M. Puthenparampil et al.   Journal of Neuroinflammation

Ocrelizumab and Other CD20+ B-Cell-Depleting Therapies in Multiple Sclerosis

(2017) Jeffrey M. Gelfand et al.   Neurotherapeutics

Ocrelizumab versus Interferon Beta-1a in Relapsing Multiple Sclerosis

(2017) Stephen L. Hauser et al.   NEW ENGLAND JOURNAL OF MEDICINE

Ocrelizumab versus Placebo in Primary Progressive Multiple Sclerosis

(2017) Xavier Montalban et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mediation of transitional B cell maturation in the absence of functional Bruton’s tyrosine kinase

(2017) Shalini Tanwar et al.   Scientific Reports

Slow expansion of multiple sclerosis iron rim lesions: pathology and 7 T magnetic resonance imaging

(2016) Assunta Dal-Bianco et al.   ACTA NEUROPATHOLOGICA

An updated histological classification system for multiple sclerosis lesions

(2016) Tanja Kuhlmann et al.   ACTA NEUROPATHOLOGICA

Targeted Covalent Inhibitors for Drug Design

(2016) Thomas A. Baillie   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Persistent 7-tesla phase rim predicts poor outcome in new multiple sclerosis patient lesions

(2016) Martina Absinta et al.   JOURNAL OF CLINICAL INVESTIGATION

Enhanced Expression of Bruton’s Tyrosine Kinase in B Cells Drives Systemic Autoimmunity by Disrupting T Cell Homeostasis

(2016) Odilia B. J. Corneth et al.   JOURNAL OF IMMUNOLOGY

Neuroinflammation: the devil is in the details

(2016) Damon J. DiSabato et al.   JOURNAL OF NEUROCHEMISTRY

Autoantibody-boosted T-cell reactivation in the target organ triggers manifestation of autoimmune CNS disease

(2016) Anne-Christine Flach et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Insufficient disease inhibition by intrathecal rituximab in progressive multiple sclerosis

(2016) Mika Komori et al.   Annals of Clinical and Translational Neurology

Clinical and pathological insights into the dynamic nature of the white matter multiple sclerosis plaque

(2015) Josa M. Frischer et al.   ANNALS OF NEUROLOGY

Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

(2015) Renato A. Bauer   DRUG DISCOVERY TODAY

CD19 differentially regulates BCR signalling through the recruitment of PI3K

(2014) Yuekang Xu et al.   AUTOIMMUNITY

Dual Functions of Bruton's Tyrosine Kinase and Tec Kinase during Fc  Receptor-Induced Signaling and Phagocytosis

(2014) J. Jongstra-Bilen et al.   JOURNAL OF IMMUNOLOGY

Ibrutinib-induced lymphocytosis in patients with chronic lymphocytic leukemia: correlative analyses from a phase II study

(2014) S E M Herman et al.   LEUKEMIA

Bruton’s Tyrosine Kinase Mediates the Synergistic Signalling between TLR9 and the B Cell Receptor by Regulating Calcium and Calmodulin

(2013) Elaine F. Kenny et al.   PLoS One

The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia

(2012) M. F. M. de Rooij et al.   BLOOD

Btk levels set the threshold for B-cell activation and negative selection of autoreactive B cells in mice

(2012) L. P. Kil et al.   BLOOD

Meningeal inflammation plays a role in the pathology of primary progressive multiple sclerosis

(2012) Sung R. Choi et al.   BRAIN

CXCL13 is the major determinant for B cell recruitment to the CSF during neuroinflammation

(2012) Markus C Kowarik et al.   Journal of Neuroinflammation

Emerging roles of endothelial cells in multiple sclerosis pathophysiology and therapy

(2012) Alireza Minagar et al.   NEUROLOGICAL RESEARCH

Bruton's tyrosine kinase phosphorylates Toll-like receptor 3 to initiate antiviral response

(2012) K.-G. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tec family kinases: regulation of FcεRI-mediated mast-cell activation

(2011) Wilfried Ellmeier et al.   FEBS Journal

NFATc1 affects mouse splenic B cell function by controlling the calcineurin–NFAT signaling network

(2011) Sankar Bhattacharyya et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Intracellular MHC class II molecules promote TLR-triggered innate immune responses by maintaining activation of the kinase Btk

(2011) Xingguang Liu et al.   NATURE IMMUNOLOGY

The Structural Biology of Toll-like Receptors

(2011) Istvan Botos et al.   STRUCTURE

Syk mediates BCR- and CD40-signaling integration during B cell activation

(2010) Haiyan Ying et al.   IMMUNOBIOLOGY

Adaptive immunity

(2010) Francisco A. Bonilla et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

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

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

IP3 Receptors: Toward Understanding Their Activation

(2010) C. W. Taylor et al.   Cold Spring Harbor Perspectives in Biology

Rituximab in patients with primary progressive multiple sclerosis: Results of a randomized double-blind placebo-controlled multicenter trial

(2009) Kathleen Hawker et al.   ANNALS OF NEUROLOGY

Microglial Physiology: Unique Stimuli, Specialized Responses

(2009) Richard M. Ransohoff et al.   Annual Review of Immunology

Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening

(2009) Róbert Kiss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

(2009) Abdalla J. Mohamed et al.   IMMUNOLOGICAL REVIEWS

Roles of the NF- B Pathway in Lymphocyte Development and Function

(2009) S. Gerondakis et al.   Cold Spring Harbor Perspectives in Biology

Erk Kinases Link Pre-B Cell Receptor Signaling to Transcriptional Events Required for Early B Cell Expansion

(2008) Tomoharu Yasuda et al.   IMMUNITY

Clinical and Molecular Analysis of 49 Patients With X-linked Agammaglobulinemia From A Single Center in Argentina

(2008) Natalia Basile et al.   JOURNAL OF CLINICAL IMMUNOLOGY

B-Cell Depletion with Rituximab in Relapsing–Remitting Multiple Sclerosis

(2008) Stephen L. Hauser et al.   NEW ENGLAND JOURNAL OF MEDICINE