- Home
- Publications
- Publication Search
- Publication Details
Title
A Comprehensive Overview of Globally Approved JAK Inhibitors
Authors
Keywords
-
Journal
Pharmaceutics
Volume 14, Issue 5, Pages 1001
Publisher
MDPI AG
Online
2022-05-09
DOI
10.3390/pharmaceutics14051001
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- Tofacitinib for the treatment of active ankylosing spondylitis in adults
- (2022) Raagav Mohanakrishnan et al. Expert Review of Clinical Immunology
- Comparing available JAK inhibitors for treating patients with psoriasis
- (2022) Parker J. Funk et al. Expert Review of Clinical Immunology
- Janus kinase-targeting therapies in rheumatology: a mechanisms-based approach
- (2022) Yoshiya Tanaka et al. Nature Reviews Rheumatology
- Covid-19: WHO recommends baricitinib and sotrovimab to treat patients
- (2022) Zosia Kmietowicz BMJ-British Medical Journal
- The Safety and Efficacy of Tofacitinib in 24 Cases of Pediatric Rheumatic Diseases: Single Centre Experience
- (2022) Mikhail M. Kostik et al. Frontiers in Pediatrics
- Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases
- (2021) Zhouling Xie et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof
- (2021) Ryan R. Davis et al. JOURNAL OF MEDICINAL CHEMISTRY
- Stereocontrolled Synthesis of Delgocitinib, a JAK Inhibitor for the Treatment of Atopic Dermatitis
- (2021) Hiromu Takiguchi et al. ORGANIC PROCESS RESEARCH & DEVELOPMENT
- The Effectiveness of Ruxolitinib for Acute/Chronic Graft-versus-Host Disease in Children: A Retrospective Study
- (2021) Wenli Yang et al. Drug Design Development and Therapy
- The Association Between the Use of Oclacitinib and Antibacterial Therapy in Dogs With Allergic Dermatitis: A Retrospective Case-Control Study
- (2021) Hester Rynhoud et al. Frontiers in Veterinary Science
- Safety and Effectiveness of Peficitinib (ASP015K) in Patients with Rheumatoid Arthritis: Final Results (32 Months of Mean Peficitinib Treatment) From a Long-Term, Open-Label Extension Study in Japan, Korea, and Taiwan
- (2021) Tsutomu Takeuchi et al. Rheumatology and Therapy
- Effects of Hepatic Impairment on the Pharmacokinetics of Abrocitinib and Its Metabolites
- (2021) Ellen Q. Wang et al. JOURNAL OF CLINICAL PHARMACOLOGY
- Synthetic Approaches to the New Drugs Approved during 2019
- (2021) Andrew C. Flick et al. JOURNAL OF MEDICINAL CHEMISTRY
- Efficacy and Safety of Ruxolitinib Cream for the Treatment of Atopic Dermatitis: Results From Two Phase 3, Randomized, Double-Blind Studies
- (2021) Kim Papp et al. JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY
- Trial of Upadacitinib and Adalimumab for Psoriatic Arthritis
- (2021) Iain B. McInnes et al. NEW ENGLAND JOURNAL OF MEDICINE
- Abrocitinib versus Placebo or Dupilumab for Atopic Dermatitis
- (2021) Thomas Bieber et al. NEW ENGLAND JOURNAL OF MEDICINE
- Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia
- (2021) Yunchao Chang et al. BLOOD
- Upadacitinib Pharmacokinetics and Exposure‐Response Analyses of Efficacy and Safety in Psoriatic Arthritis Patients – Analyses of Phase 3 Clinical Trials
- (2021) Elena Muensterman et al. CTS-Clinical and Translational Science
- A phase 2 multiple ascending dose study of the inhaled pan-JAK inhibitor nezulcitinib (TD–0903) in severe COVID-19
- (2021) Dave Singh et al. EUROPEAN RESPIRATORY JOURNAL
- Safety of Janus kinase (JAK) inhibitors in the short‐term treatment of atopic dermatitis
- (2021) Hannah Wood et al. INTERNATIONAL JOURNAL OF DERMATOLOGY
- Abrocitinib induction, randomized withdrawal, and retreatment in patients with moderate-to-severe atopic dermatitis: Results from the JAK1 Atopic Dermatitis Efficacy and Safety (JADE) REGIMEN phase 3 trial
- (2021) Andrew Blauvelt et al. JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY
- Filgotinib as induction and maintenance therapy for ulcerative colitis (SELECTION): a phase 2b/3 double-blind, randomised, placebo-controlled trial
- (2021) Brian G Feagan et al. LANCET
- Tofacitinib in Patients Hospitalized with Covid-19 Pneumonia
- (2021) Patrícia O. Guimarães et al. NEW ENGLAND JOURNAL OF MEDICINE
- Deep learning identifies synergistic drug combinations for treating COVID-19
- (2021) Wengong Jin et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Efficacy and Safety of Abrocitinib in Combination With Topical Therapy in Adolescents With Moderate-to-Severe Atopic Dermatitis
- (2021) Lawrence F. Eichenfield et al. JAMA Dermatology
- Efficacy and Safety of Upadacitinib vs Dupilumab in Adults With Moderate-to-Severe Atopic Dermatitis
- (2021) Andrew Blauvelt et al. JAMA Dermatology
- Efficacy and safety of baricitinib for the treatment of hospitalised adults with COVID-19 (COV-BARRIER): a randomised, double-blind, parallel-group, placebo-controlled phase 3 trial
- (2021) Vincent C Marconi et al. Lancet Respiratory Medicine
- Clinical impact of combination therapy with baricitinib, remdesivir, and dexamethasone in patients with severe COVID-19
- (2021) Takehiro Izumo et al. Respiratory Investigation
- Economic Benefit from Improvements in Quality of Life with Upadacitinib: Comparisons with Tofacitinib and Methotrexate in Patients with Rheumatoid Arthritis
- (2021) Martin Bergman et al. ADVANCES IN THERAPY
- Abrocitinib: First Approval
- (2021) Emma D. Deeks et al. DRUGS
- Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis
- (2021) Cecilia C. Ayala-Aguilera et al. JOURNAL OF MEDICINAL CHEMISTRY
- Icotinib, Almonertinib, and Olmutinib: A 2D Similarity/Docking-Based Study to Predict the Potential Binding Modes and Interactions into EGFR
- (2021) Faisal A. Almalki et al. MOLECULES
- Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism
- (2021) Mohammed A. S. Abourehab et al. MOLECULES
- Pyrrolizine/Indolizine-NSAID Hybrids: Design, Synthesis, Biological Evaluation, and Molecular Docking Studies
- (2021) Mohammed A. S. Abourehab et al. MOLECULES
- Immunomodulatory effect of long‐term oclacitinib maleate therapy in dogs with atopic dermatitis
- (2021) Guilherme Caro Martins et al. VETERINARY DERMATOLOGY
- Jakinibs of All Trades: Inhibiting Cytokine Signaling in Immune-Mediated Pathologies
- (2021) Madison Alexander et al. Pharmaceuticals
- Safety Profile of Upadacitinib up to 3 Years in Psoriatic Arthritis: An Integrated Analysis of Two Pivotal Phase 3 Trials
- (2021) Gerd R. Burmester et al. Rheumatology and Therapy
- Improvement in Patient-Reported Outcomes in Patients with Psoriatic Arthritis Treated with Upadacitinib Versus Placebo or Adalimumab: Results from SELECT-PsA 1
- (2021) Vibeke Strand et al. Rheumatology and Therapy
- Do JAK inhibitors affect immune response to COVID-19 vaccination? Data from the MAJIK-SFR Registry
- (2021) Raphaèle Seror et al. Lancet Rheumatology
- JAK Inhibitors for Treatment of Psoriasis: Focus on Selective TYK2 Inhibitors
- (2020) Miguel Nogueira et al. DRUGS
- Delgocitinib ointment, a topical Janus kinase inhibitor, in adult patients with moderate to severe atopic dermatitis: A phase 3, randomized, double-blind, vehicle-controlled study and an open-label, long-term extension study
- (2020) Hidemi Nakagawa et al. JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY
- Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1
- (2020) Andrew Fensome et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Delgocitinib: First Approval
- (2020) Sohita Dhillon DRUGS
- Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders
- (2020) Pengfei Xu et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Peficitinib for the treatment of rheumatoid arthritis: an overview from clinical trials
- (2020) Yoshiya Tanaka et al. EXPERT OPINION ON PHARMACOTHERAPY
- A TYK2 Gene Mutation c.2395G>A Leads to TYK2 Deficiency: A Case Report and Literature Review
- (2020) Peilin Wu et al. Frontiers in Pediatrics
- Excretion balance and pharmacokinetics following a single oral dose of [14C]-fedratinib in healthy subjects
- (2020) Ken Ogasawara et al. CANCER CHEMOTHERAPY AND PHARMACOLOGY
- Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders
- (2020) Satoru Noji et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fedratinib, a newly approved treatment for patients with myeloproliferative neoplasm-associated myelofibrosis
- (2020) Moshe Talpaz et al. LEUKEMIA
- Efficacy and safety of peficitinib in rheumatoid arthritis
- (2020) Yuko Kaneko Modern Rheumatology
- Inside Perspective of the Synthetic and Computational Toolbox of JAK Inhibitors: Recent Updates
- (2020) Adriana Coricello et al. MOLECULES
- The Generation of an Engineered Interleukin-10 Protein With Improved Stability and Biological Function
- (2020) Faisal Minshawi et al. Frontiers in Immunology
- JAK-Inhibitors for the Treatment of Rheumatoid Arthritis: A Focus on the Present and an Outlook on the Future
- (2020) Jacopo Angelini et al. Biomolecules
- A phase 1 trial of itacitinib, a selective JAK1 inhibitor, in patients with acute graft-versus-host disease
- (2020) Mark A. Schroeder et al. Blood Advances
- Development of a Nitrene-Type Rearrangement for the Commercial Route of the JAK1 Inhibitor Abrocitinib
- (2020) Christina G. Connor et al. ORGANIC PROCESS RESEARCH & DEVELOPMENT
- Filgotinib: First Approval
- (2020) Sohita Dhillon et al. DRUGS
- Baricitinib plus Remdesivir for Hospitalized Adults with Covid-19
- (2020) Andre C. Kalil et al. NEW ENGLAND JOURNAL OF MEDICINE
- Additional baricitinib loading dose improves clinical outcome in COVID-19
- (2020) Md Jahidul Hasan et al. Open Medicine
- JAK1 inhibition and inflammatory bowel disease
- (2020) Clare Harris et al. RHEUMATOLOGY
- Selective Janus kinase inhibitors come of age
- (2019) John J. O’Shea et al. Nature Reviews Rheumatology
- Selective JAKinibs: Prospects in Inflammatory and Autoimmune Diseases
- (2019) Anniina T. Virtanen et al. BIODRUGS
- Peficitinib: First Global Approval
- (2019) Anthony Markham et al. DRUGS
- Preclinical activity and a pilot phase I study of pacritinib, an oral JAK2/FLT3 inhibitor, and chemotherapy in FLT3-ITD-positive AML
- (2019) Jae Yoon Jeon et al. INVESTIGATIONAL NEW DRUGS
- Upadacitinib as monotherapy in patients with active rheumatoid arthritis and inadequate response to methotrexate (SELECT-MONOTHERAPY): a randomised, placebo-controlled, double-blind phase 3 study
- (2019) Josef S Smolen et al. LANCET
- Tofacitinib Treatment of Refractory Systemic Juvenile Idiopathic Arthritis
- (2019) Zhixiang Huang et al. PEDIATRICS
- Tofacitinib Trial Prompts FDA Review of Adverse Effects
- (2019) Diane S. Aschenbrenner AMERICAN JOURNAL OF NURSING
- Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling
- (2019) Mark Zak et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
- (2019) Stephen T. Wrobleski et al. JOURNAL OF MEDICINAL CHEMISTRY
- Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain
- (2019) James R. Burke et al. Science Translational Medicine
- FLT3 overexpression in acute leukaemias: New insights into the search for molecular mechanisms
- (2019) Caroline Pires Poubel et al. BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER
- Efficacy and safety of topical delgocitinib in patients with chronic hand eczema: data from a randomised, double‐blind, vehicle‐controlled Phase 2a study
- (2019) M. Worm et al. BRITISH JOURNAL OF DERMATOLOGY
- Tofacitinib Is a Mechanism-Based Inactivator of Cytochrome P450 3A4
- (2019) Xiucai Guo et al. CHEMICAL RESEARCH IN TOXICOLOGY
- Fedratinib: First Approval
- (2019) Hannah A. Blair DRUGS
- Upadacitinib: First Approval
- (2019) Sean Duggan et al. DRUGS
- Treatment of atopic dermatitis with ruxolitinib cream (JAK1/JAK2 inhibitor) or triamcinolone cream
- (2019) Brian S. Kim et al. JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
- Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms
- (2019) Tao Yang et al. JOURNAL OF MEDICINAL CHEMISTRY
- FDA Approval Summary: Ruxolitinib for Treatment of Steroid‐Refractory Acute Graft‐Versus‐Host Disease
- (2019) Donna Przepiorka et al. ONCOLOGIST
- Enzymatic Characterization of Wild-Type and Mutant Janus Kinase 1
- (2019) Nicholas P. D. Liau et al. Cancers
- Clinical Pharmacokinetics of Upadacitinib: Review of Data Relevant to the Rheumatoid Arthritis Indication
- (2019) Mohamed-Eslam F. Mohamed et al. CLINICAL PHARMACOKINETICS
- Molecular structure and function of Janus kinases: implications for the development of inhibitors
- (2019) Alba Garrido-Trigo et al. Journal of Crohns & Colitis
- Pharmacokinetics and Safety of a Single Oral Dose of Peficitinib (ASP015K) in Japanese Subjects With Normal and Impaired Hepatic Function
- (2019) Daisuke Miyatake et al. Clinical Pharmacology in Drug Development
- An Update on JAK Inhibitors
- (2018) Francesca Musumeci et al. CURRENT MEDICINAL CHEMISTRY
- The regulation of JAKs in cytokine signaling and its breakdown in disease
- (2018) Henrik M. Hammarén et al. CYTOKINE
- Baricitinib: A Review in Rheumatoid Arthritis
- (2018) Zaina T. Al-Salama et al. DRUGS
- Filgotinib for the treatment of Crohn’s disease
- (2018) Remi Labetoulle et al. EXPERT OPINION ON INVESTIGATIONAL DRUGS
- Phase 1 studies to assess the safety, tolerability and pharmacokinetics of JTE-052 (a novel Janus kinase inhibitor) ointment in Japanese healthy volunteers and patients with atopic dermatitis
- (2018) Hidemi Nakagawa et al. JOURNAL OF DERMATOLOGY
- Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances
- (2018) Marian C. Bryan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
- (2018) Michael L. Vazquez et al. JOURNAL OF MEDICINAL CHEMISTRY
- Baricitinib in adult patients with moderate-to-severe atopic dermatitis: a phase 2 parallel, double-blinded, randomized placebo-controlled multiple-dose study
- (2018) Emma Guttman-Yassky et al. JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY
- Baricitinib for systemic lupus erythematosus: a double-blind, randomised, placebo-controlled, phase 2 trial
- (2018) Daniel J Wallace et al. LANCET
- Inhibition of interleukin-1 receptor-associated kinase-1 is a therapeutic strategy for acute myeloid leukemia subtypes
- (2018) Mona M. Hosseini et al. LEUKEMIA
- Compound heterozygous TYK2 mutations underlie primary immunodeficiency with T-cell lymphopenia
- (2018) Michiko Nemoto et al. Scientific Reports
- Pacritinib vs Best Available Therapy, Including Ruxolitinib, in Patients With Myelofibrosis
- (2018) John Mascarenhas et al. JAMA Oncology
- Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor
- (2018) Hisao Hamaguchi et al. BIOORGANIC & MEDICINAL CHEMISTRY
- A Dual Inhibition, a Better Solution: Development of a JAK1/TYK2 inhibitor
- (2018) Christel J Menet JOURNAL OF MEDICINAL CHEMISTRY
- Upadacitinib for the treatment of rheumatoid arthritis
- (2018) Lina Serhal et al. Expert Review of Clinical Immunology
- Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
- (2018) Agustin Casimiro-Garcia et al. JOURNAL OF MEDICINAL CHEMISTRY
- Efficacy and safety of filgotinib, a selective Janus kinase 1 inhibitor, in patients with active psoriatic arthritis (EQUATOR): results from a randomised, placebo-controlled, phase 2 trial
- (2018) Philip Mease et al. LANCET
- Immunomodulatory in vitro effects of oclacitinib on canine T-cell proliferation and cytokine production
- (2018) Frane Banovic et al. VETERINARY DERMATOLOGY
- JAK1 somatic mutation in a myeloproliferative neoplasm
- (2017) Suzanne O. Arulogun et al. HAEMATOLOGICA
- A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model
- (2017) Misato Ito et al. JOURNAL OF PHARMACOLOGICAL SCIENCES
- Clinical remission in patients with moderate-to-severe Crohn's disease treated with filgotinib (the FITZROY study): results from a phase 2, double-blind, randomised, placebo-controlled trial
- (2017) Séverine Vermeire et al. LANCET
- Rethinking JAK2 inhibition: towards novel strategies of more specific and versatile janus kinase inhibition
- (2017) E Leroy et al. LEUKEMIA
- A phase 1 study of the Janus kinase 2 ( JAK2 ) V617F inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia
- (2017) Srdan Verstovsek et al. LEUKEMIA RESEARCH
- JAK inhibition as a therapeutic strategy for immune and inflammatory diseases
- (2017) Daniella M. Schwartz et al. NATURE REVIEWS DRUG DISCOVERY
- Tofacitinib or Adalimumab versus Placebo for Psoriatic Arthritis
- (2017) Philip Mease et al. NEW ENGLAND JOURNAL OF MEDICINE
- Tofacitinib for Psoriatic Arthritis in Patients with an Inadequate Response to TNF Inhibitors
- (2017) Dafna Gladman et al. NEW ENGLAND JOURNAL OF MEDICINE
- The JAK2/STAT3 inhibitor pacritinib effectively inhibits patient-derived GBM brain tumor initiating cells in vitro and when used in combination with temozolomide increases survival in an orthotopic xenograft model
- (2017) Katharine Victoria Jensen et al. PLoS One
- The target landscape of clinical kinase drugs
- (2017) Susan Klaeger et al. SCIENCE
- JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules
- (2017) Ana S. Newton et al. ACS Medicinal Chemistry Letters
- JAK1 somatic mutation in a myeloproliferative neoplasm
- (2017) Suzanne O. Arulogun et al. HAEMATOLOGICA
- Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK-1 Inhibitor, After Short-Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials
- (2017) Frédéric Vanhoutte et al. Arthritis & Rheumatology
- Peficitinib, a JAK Inhibitor, in Combination With Limited Conventional Synthetic Disease-Modifying Antirheumatic Drugs in the Treatment of Moderate-to-Severe Rheumatoid Arthritis
- (2017) Mark C. Genovese et al. Arthritis & Rheumatology
- Pacritinib versus best available therapy for the treatment of myelofibrosis irrespective of baseline cytopenias (PERSIST-1): an international, randomised, phase 3 trial
- (2017) Ruben A Mesa et al. Lancet Haematology
- The Janus Kinase (JAK) FERM and SH2 Domains: Bringing Specificity to JAK–Receptor Interactions
- (2017) Ryan Ferrao et al. Frontiers in Endocrinology
- Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition
- (2016) Jean-Baptiste Telliez et al. ACS Chemical Biology
- Filgotinib (GLPG0634/GS-6034), an oral JAK1 selective inhibitor, is effective in combination with methotrexate (MTX) in patients with active rheumatoid arthritis and insufficient response to MTX: results from a randomised, dose-finding study (DARWIN 1)
- (2016) R Westhovens et al. ANNALS OF THE RHEUMATIC DISEASES
- Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis
- (2016) Mohamed-Eslam F. Mohamed et al. CLINICAL PHARMACOKINETICS
- Hyperactivation of JAK1 tyrosine kinase induces stepwise, progressive pruritic dermatitis
- (2016) Takuwa Yasuda et al. JOURNAL OF CLINICAL INVESTIGATION
- Phase 1/2 study of pacritinib, a next generation JAK2/FLT3 inhibitor, in myelofibrosis or other myeloid malignancies
- (2016) Srdan Verstovsek et al. Journal of Hematology & Oncology
- Family-wide Structural Analysis of Human Numb-Associated Protein Kinases
- (2016) Fiona J. Sorrell et al. STRUCTURE
- An efficient synthesis of baricitinib
- (2016) Jiaojiao Xu et al. JOURNAL OF CHEMICAL RESEARCH
- Rationally Repurposing Ruxolitinib (Jakafi®) as a Solid Tumor Therapeutic
- (2016) Mehrad Tavallai et al. Frontiers in Oncology
- Regio- and Enantioselective Synthesis of N-Substituted Pyrazoles by Rhodium-Catalyzed Asymmetric Addition to Allenes
- (2015) Alexander M. Haydl et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study
- (2015) Tsutomu Takeuchi et al. ANNALS OF THE RHEUMATIC DISEASES
- Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia
- (2015) Shuo-Chieh Wu et al. CANCER CELL
- Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection
- (2015) Florence Namour et al. CLINICAL PHARMACOKINETICS
- Efficacy and safety of ruxolitinib in the treatment of patients with myelofibrosis
- (2015) Cecilia Arana Yi et al. Future Oncology
- Structural and Functional Characterization of the JH2 Pseudokinase Domain of JAK Family Tyrosine Kinase 2 (TYK2)
- (2015) Xiaoshan Min et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Development of Selective Covalent Janus Kinase 3 Inhibitors
- (2015) Li Tan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Targeting JAK kinase in solid tumors: emerging opportunities and challenges
- (2015) M Buchert et al. ONCOGENE
- Human mass balance, metabolite profile and identification of metabolic enzymes of [14C]ASP015K, a novel oral janus kinase inhibitor
- (2015) Kazuo Oda et al. XENOBIOTICA
- Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma
- (2015) Jiao Ma et al. Oncotarget
- VX-509 (Decernotinib), an Oral Selective JAK-3 Inhibitor, in Combination With Methotrexate in Patients With Rheumatoid Arthritis
- (2015) Mark C. Genovese et al. Arthritis & Rheumatology
- Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol
- (2015) Eric R. Goedken et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
- (2014) Stuart W. J. Ember et al. ACS Chemical Biology
- Selective JAK inhibitors in development for rheumatoid arthritis
- (2014) Peter Norman EXPERT OPINION ON INVESTIGATIONAL DRUGS
- Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo
- (2014) Atsuo Tanimoto et al. INFLAMMATION RESEARCH
- Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634
- (2014) Christel J. Menet et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases
- (2014) James D. Clark et al. JOURNAL OF MEDICINAL CHEMISTRY
- Oclacitinib (APOQUEL®) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy
- (2014) A. J. Gonzales et al. JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
- Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
- (2014) Pietro Ciceri et al. Nature Chemical Biology
- c-Src Binds to the Cancer Drug Ruxolitinib with an Active Conformation
- (2014) Yankun Duan et al. PLoS One
- Crystal Structures of PRK1 in Complex with the Clinical Compounds Lestaurtinib and Tofacitinib Reveal Ligand Induced Conformational Changes
- (2014) Philip Chamberlain et al. PLoS One
- Tofacitinib (CP-690,550) in patients with rheumatoid arthritis receiving methotrexate: Twelve-month data from a twenty-four-month phase III randomized radiographic study
- (2013) Désirée van der Heijde et al. ARTHRITIS AND RHEUMATISM
- Therapeutic Targeting of the JAK/STAT Pathway
- (2013) Saara Aittomäki et al. BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
- JAK Inhibitors: Pharmacology and Clinical Activity in Chronic Myeloprolipherative Neoplasms
- (2013) J. Trelinski et al. CURRENT MEDICINAL CHEMISTRY
- Preclinical Characterization of GLPG0634, a Selective Inhibitor of JAK1, for the Treatment of Inflammatory Diseases
- (2013) L. Van Rompaey et al. JOURNAL OF IMMUNOLOGY
- The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog
- (2013) W. T. Collard et al. JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
- Myelofibrosis, JAK2 inhibitors and erythropoiesis
- (2013) W Vainchenker et al. LEUKEMIA
- Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348)
- (2013) T Zhou et al. LEUKEMIA
- Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis
- (2013) Sallie B. Cosgrove et al. VETERINARY DERMATOLOGY
- Ruxolitinib: The First FDA Approved Therapy for the Treatment of Myelofibrosis
- (2012) J. Mascarenhas et al. CLINICAL CANCER RESEARCH
- Biology and significance of the JAK/STAT signalling pathways
- (2012) Hiu Kiu et al. GROWTH FACTORS
- Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis
- (2012) Roy Fleischmann et al. NEW ENGLAND JOURNAL OF MEDICINE
- Tofacitinib or Adalimumab versus Placebo in Rheumatoid Arthritis
- (2012) Ronald F. van Vollenhoven et al. NEW ENGLAND JOURNAL OF MEDICINE
- A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis
- (2012) Srdan Verstovsek et al. NEW ENGLAND JOURNAL OF MEDICINE
- Tofacitinib, an Oral Janus Kinase Inhibitor, in Active Ulcerative Colitis
- (2012) William J. Sandborn et al. NEW ENGLAND JOURNAL OF MEDICINE
- Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
- (2012) Rita Andraos et al. Cancer Discovery
- Bromodomains as therapeutic targets
- (2011) Susanne Muller et al. EXPERT REVIEWS IN MOLECULAR MEDICINE
- The Effect of CYP3A4 Inhibition or Induction on the Pharmacokinetics and Pharmacodynamics of Orally Administered Ruxolitinib (INCB018424 Phosphate) in Healthy Volunteers
- (2011) Jack G. Shi et al. JOURNAL OF CLINICAL PHARMACOLOGY
- Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-Like Tyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma
- (2011) Anthony D. William et al. JOURNAL OF MEDICINAL CHEMISTRY
- Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia
- (2011) S Hart et al. Blood Cancer Journal
- Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms
- (2010) A. Quintas-Cardama et al. BLOOD
- Metabolism, Excretion, and Pharmacokinetics of [14C]INCB018424, a Selective Janus Tyrosine Kinase 1/2 Inhibitor, in Humans
- (2010) A. D. Shilling et al. DRUG METABOLISM AND DISPOSITION
- The JAK2 V617F somatic mutation, mortality and cancer risk in the general population
- (2010) C. Nielsen et al. HAEMATOLOGICA
- Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family
- (2010) Gebhard Thoma et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural and Thermodynamic Characterization of the TYK2 and JAK3 Kinase Domains in Complex with CP-690550 and CMP-6
- (2010) Jill E. Chrencik et al. JOURNAL OF MOLECULAR BIOLOGY
- Dissecting Specificity in the Janus Kinases: The Structures of JAK-Specific Inhibitors Complexed to the JAK1 and JAK2 Protein Tyrosine Kinase Domains
- (2009) Neal K. Williams et al. JOURNAL OF MOLECULAR BIOLOGY
- CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients
- (2009) A Pardanani et al. LEUKEMIA
- Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction
- (2009) Qiyan Lin et al. ORGANIC LETTERS
- Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera
- (2008) Gerlinde Wernig et al. CANCER CELL
- JAK2 and MPL mutations in myeloproliferative neoplasms: discovery and science
- (2008) O Kilpivaara et al. LEUKEMIA
- LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells
- (2008) D. B. Lipka et al. MOLECULAR CANCER THERAPEUTICS
Add your recorded webinar
Do you already have a recorded webinar? Grow your audience and get more views by easily listing your recording on Peeref.
Upload NowAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started