skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Discovery of BIIB068: A Selective, Potent, Reversible Bruton?s Tyrosine Kinase Inhibitor as an Orall

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1836743
Journal Information:
J. Med. Chem., Vol. 63, Issue (21)
Country of Publication:
United States
Language:
ENGLISH

References (56)

Targeting pathological B cell receptor signalling in lymphoid malignancies journal March 2013
Bruton’s Tyrosine Kinase: An Emerging Key Player in Innate Immunity journal November 2017
The Bruton's tyrosine kinase gene is expressed throughout B cell differentiation, from early precursor B cell stages preceding immunoglobulin gene rearrangement up to mature B cell stages journal December 1993
X-Linked Agammaglobulinemia and Other Immunoglobulin Deficiencies journal April 1994
Analysis of Clinical Presentations of Bruton Disease: A Review of 20 Years of Accumulated Data from Pediatric Patients at Severance Hospital journal January 2008
Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia journal January 1993
The gene involved in X-linked agammaglobulinaemia is a member of the src family of protein-tyrosine kinases journal January 1993
Role of Bruton's tyrosine kinase in immunodeficiency journal August 1994
X-linked immunodeficient mice spontaneously produce lupus-related anti-RNA helicase A autoantibodies, but are resistant to pristane-induced lupus journal September 2003
The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy journal July 2010
Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell–associated damage in IFNα-driven lupus nephritis journal April 2017
The Role of Tec Family Kinases in Myeloid Cells journal January 2004
Inhibiting Bruton’s tyrosine kinase rescues mice from lethal influenza-induced acute lung injury journal July 2018
BTK inhibition is a potent approach to block IgE‐mediated histamine release in human basophils journal April 2017
Analysis of the Effects of the Bruton's tyrosine kinase (Btk) Inhibitor Ibrutinib on Monocyte Fcγ Receptor (FcγR) Function journal February 2016
Ibrutinib and novel BTK inhibitors in clinical development journal January 2013
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review journal May 2018
New therapies for systemic lupus erythematosus — past imperfect, future tense journal June 2019
Role of Bruton’s tyrosine kinase in B cells and malignancies journal February 2018
Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor journal March 2016
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal August 2019
Second-generation inhibitors of Bruton tyrosine kinase journal September 2016
Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis journal June 2019
Ibrutinib in CLL: a focus on adverse events, resistance, and novel approaches beyond ibrutinib journal March 2017
Idiosyncratic Toxicity: A Convergence of Risk Factors journal February 2007
Inhibition of Btk with CC-292 Provides Early Pharmacodynamic Assessment of Activity in Mice and Humans journal May 2013
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinase (BTK) journal March 2019
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases journal August 2019
A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers: A phase I study of PRN1008 journal August 2017
Bruton’s tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018) journal March 2019
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal February 2020
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development journal February 2018
Discovery of 6-Fluoro-5-( R )-(3-( S )-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4 H )-yl)-2-methylphenyl)-2-( S )-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1 H -carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers journal September 2016
Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton’s Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis journal September 2018
Op0025 Fenebrutinib Compared to Placebo and Adalimumab in Patients with Inadequate Response to Either Methotrexate Therapy or Prior tnf Therapy: Phase 2 Study conference June 2019
Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis journal January 2020
Spebrutinib (CC-292) Affects Markers of B Cell Activation, Chemotaxis, and Osteoclasts in Patients with Rheumatoid Arthritis: Results from a Mechanistic Study journal November 2019
Sat0089 Safety and Efficacy of Ly3337641, a Bruton’S Tyrosine Kinase Inhibitor in Patients with Rheumatoid Arthritis: a Randomized, Double-Blind, Placebo-Controlled, 2-Part Phase 2 Study conference June 2019
Optimization of novel reversible Bruton’s tyrosine kinase inhibitors identified using Tethering-fragment-based screens journal July 2019
Ability of Bruton’s Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling journal January 2017
Specific Btk inhibition suppresses B cell– and myeloid cell–mediated arthritis journal November 2010
Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling journal April 2019
Building Predictive Models for Mechanism-of-Action Classification from Phenotypic Assay Data Sets journal October 2013
Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models journal April 2019
Palladium-Catalyzed Cross-Coupling Reactions of Organoboron Compounds journal November 1995
Monodentate Phosphines Provide Highly Active Catalysts for Pd-Catalyzed CN Bond-Forming Reactions of Heteroaromatic Halides/Amines and (H)N-Heterocycles journal October 2006
Defective B cell development and function in Btk-deficient mice journal September 1995
ABBV-105, a selective and irreversible inhibitor of Bruton’s tyrosine kinase, is efficacious in multiple preclinical models of inflammation journal July 2018
Correction of the X-linked immunodeficiency phenotype by transgenic expression of human Bruton tyrosine kinase under the control of the class II major histocompatibility complex Ea locus control region journal January 1997
Mechanistic Investigations of Test Article–Induced Pancreatic Toxicity at the Endocrine–Exocrine Interface in the Rat journal November 2013
Long-term therapy with sorafenib is associated with pancreatic atrophy journal December 2015
Bruton’s Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats journal November 2016
Pancreatic Effects of a Bruton’s Tyrosine Kinase Small-molecule Inhibitor in Rats Are Strain-dependent journal April 2018
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 journal April 2011
Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases: Crystal Structures of Human BTK Kinase Domain journal January 2010
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010

Similar Records

Discovery of BIIB068: A Selective, Potent, Reversible Bruton?s Tyrosine Kinase Inhibitor as an Orall
Journal Article · Wed Jul 01 00:00:00 EDT 2020 · J. Med. Chem. · OSTI ID:1836743

Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton?s Tyrosine Kinase
Journal Article · Sat Oct 01 00:00:00 EDT 2022 · J. Med. Chem. · OSTI ID:1836743

Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834
Journal Article · Sun Mar 01 00:00:00 EST 2015 · Bioorganic and Medicinal Chemistry Letters · OSTI ID:1836743

Related Subjects