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

Immunological Diseases ◽

Bruton’s Tyrosine Kinase (BTK) Inhibitor RN486 Overcomes ABCB1-Mediated Multidrug Resistance in Cancer Cells

Frontiers in Cell and Developmental Biology ◽

10.3389/fcell.2020.00865 ◽

2020 ◽

Vol 8 ◽

Author(s):

Xing-Duo Dong ◽

Meng Zhang ◽

Xiubin Ma ◽

Jing-Quan Wang ◽

Zi-Ning Lei ◽

...

Keyword(s):

Multidrug Resistance ◽

Tyrosine Kinase ◽

Cancer Cells ◽

Abstract 3531: Changes in immune cell populations in relapsed/refractory CLL patients treated with a Bruton's Tyrosine Kinase (BTK) Inhibitor, Ibrutinib (PCI-32765), in combination with Bendamustine and Rituximab (BR).

10.1158/1538-7445.am2013-3531 ◽

2013 ◽

Author(s):

Rajendra N. Damle ◽

Sonal Temburni ◽

Prachi Aggarwal ◽

Susan O'Brien ◽

Jacqueline Barrientos ◽

...

Keyword(s):

Tyrosine Kinase ◽

Immune Cell ◽

Cell Populations ◽

Anti-tumor efficacy study of the Bruton’s tyrosine kinase (BTK) inhibitor, ONO/GS-4059, in combination with the glycoengineered type II anti-CD20 monoclonal antibody obinutuzumab (GA101) demonstrates superior in vivo efficacy compared to ONO/GS-4059 in combination with rituximab

Leukemia & Lymphoma ◽

10.1080/10428194.2016.1201567 ◽

2016 ◽

Vol 58 (3) ◽

pp. 699-707 ◽

Cited By ~ 12

Author(s):

Tomoko Yasuhiro ◽

Wako Sawada ◽

Christian Klein ◽

Ryohei Kozaki ◽

Shingo Hotta ◽

...

Keyword(s):

Monoclonal Antibody ◽

Tyrosine Kinase ◽

Efficacy Study ◽

Type Ii ◽

In Vivo Efficacy ◽

Btk Inhibitor ◽

Anti Cd20

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

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2014.11.030 ◽

2015 ◽

Vol 25 (2) ◽

pp. 367-371 ◽

Cited By ~ 24

Author(s):

Yan Lou ◽

Zachary K. Sweeney ◽

Andreas Kuglstatter ◽

Dana Davis ◽

David M. Goldstein ◽

...

Keyword(s):

Tyrosine Kinase ◽

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

Journal of Medicinal Chemistry ◽

10.1021/jm500305p ◽

2014 ◽

Vol 58 (1) ◽

pp. 512-516 ◽

Cited By ~ 56

Author(s):

Yan Lou ◽

Xiaochun Han ◽

Andreas Kuglstatter ◽

Rama K. Kondru ◽

Zachary K. Sweeney ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Drug Design ◽

Tyrosine Kinase ◽

Structure Based Drug Design ◽

BRUTON'S TYROSINE KINASE (BTK) INHIBITOR BGB-3111 DEMONSTRATES HIGH VERY GOOD PARTIAL RESPONSE (VGPR) RATE IN PATIENTS WITH WALDENSTRÖM MACROGLOBULINEMIA (WM)

Hematological Oncology ◽

10.1002/hon.2437_58 ◽

2017 ◽

Vol 35 ◽

pp. 70-71 ◽

Cited By ~ 10

Author(s):

J. Trotman ◽

S. Opat ◽

P. Marlton ◽

D. Gottlieb ◽

D. Simpson ◽

...

Keyword(s):

Partial Response ◽

Tyrosine Kinase ◽

Waldenström Macroglobulinemia ◽

Waldenstrom Macroglobulinemia ◽

Btk Inhibitor ◽

Good Partial Response

THU0194 A Novel Reversibile Bruton's Tyrosine Kinase (BTK) Inhibitor (BMS-986142) Provides Favorable Safety, Pharmacokinetic, and Pharmacodynamic Profiles in Healthy Subjects:

Annals of the Rheumatic Diseases ◽

10.1136/annrheumdis-2016-eular.3360 ◽

2016 ◽

Vol 75 (Suppl 2) ◽

pp. 256.1-256

Author(s):

S.K. Lee ◽

J. Xing ◽

I. Catlett ◽

R. Adamczyk ◽

A. Griffies ◽

...

Keyword(s):

Tyrosine Kinase ◽

Healthy Subjects ◽

Btk Inhibitor ◽

Favorable Safety

ZYBT1, a potent, irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer

Pharmacology Research & Perspectives ◽

10.1002/prp2.565 ◽

2020 ◽

Vol 8 (4) ◽

Author(s):

Krishnarup Ghoshdastidar ◽

Hoshang Patel ◽

Hitesh Bhayani ◽

Ankit Patel ◽

Kinjal Thakkar ◽

...

Keyword(s):

Tyrosine Kinase ◽

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

10.1158/1538-7445.am2015-2596 ◽

2015 ◽

Cited By ~ 18

Author(s):

Todd Covey ◽

Tjeerd Barf ◽

Michael Gulrajani ◽

Fanny Krantz ◽

Bart van Lith ◽

...

Keyword(s):

Chronic Lymphocytic Leukemia ◽

Tyrosine Kinase ◽

Lymphocytic Leukemia ◽

Target Coverage ◽

Analysis of the Effects of the Bruton's tyrosine kinase (Btk) Inhibitor Ibrutinib on Monocyte Fcγ Receptor (FcγR) Function

Journal of Biological Chemistry ◽

10.1074/jbc.m115.687251 ◽

2015 ◽

Vol 291 (6) ◽

pp. 3043-3052 ◽

Cited By ~ 30

Author(s):

Li Ren ◽

Amanda Campbell ◽

Huiqing Fang ◽

Shalini Gautam ◽

Saranya Elavazhagan ◽

...

Keyword(s):

Tyrosine Kinase ◽

Fcγ Receptor ◽