A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers

Reversible Covalent ◽

Safety, pharmacokinetics and pharmacodynamics of BI 705564, a highly selective, covalent inhibitor of Bruton's tyrosine kinase, in Phase I clinical trials in healthy volunteers

British Journal of Clinical Pharmacology ◽

10.1111/bcp.14571 ◽

2020 ◽

Author(s):

Tobias Litzenburger ◽

Jürgen Steffgen ◽

Ewald Benediktus ◽

Fabian Müller ◽

Armin Schultz ◽

...

Keyword(s):

Clinical Trials ◽

Tyrosine Kinase ◽

Phase I ◽

Healthy Volunteers ◽

Phase I Clinical Trials ◽

Pharmacokinetics And Pharmacodynamics ◽

Faculty Opinions recommendation of Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.734569206.793554988 ◽

2019 ◽

Author(s):

John Lowe

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Reactive Group ◽

Zanubrutinib (BGB-3111), a Second-Generation Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase and Its Utility in Treating Chronic Lymphocytic Leukemia

Drug Design Development and Therapy ◽

10.2147/dddt.s250823 ◽

2021 ◽

Vol Volume 15 ◽

pp. 919-926

Author(s):

Joanna M Rhodes ◽

Anthony R Mato

Keyword(s):

Chronic Lymphocytic Leukemia ◽

Tyrosine Kinase ◽

Second Generation ◽

Lymphocytic Leukemia ◽

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

Clinical Pharmacology & Therapeutics ◽

10.1002/cpt.1056 ◽

2018 ◽

Vol 103 (6) ◽

pp. 1020-1028 ◽

Cited By ~ 17

Author(s):

Ann E. Herman ◽

Leslie W. Chinn ◽

Shweta G. Kotwal ◽

Elaine R. Murray ◽

Rui Zhao ◽

...

Keyword(s):

Tyrosine Kinase ◽

Healthy Volunteers ◽

Kinase Inhibitor ◽

Pharmacokinetics And Pharmacodynamics ◽

Bruton's Tyrosine Kinase

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

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b01916 ◽

2020 ◽

Vol 63 (10) ◽

pp. 5102-5118 ◽

Cited By ~ 8

Author(s):

Daniela Angst ◽

François Gessier ◽

Philipp Janser ◽

Anna Vulpetti ◽

Rudolf Wälchli ◽

...

Keyword(s):

Tyrosine Kinase ◽

Preclinical Mechanism of Action of PRN1008, a Reversible Covalent Bruton’s Tyrosine Kinase Inhibitor in Clinical Development for Pemphigus

10.26226/morressier.5d4980c98fb7e44098e72b12 ◽

2019 ◽

Author(s):

Claire Langrish ◽

Kristin MacIntosh

Keyword(s):

Tyrosine Kinase ◽

Mechanism Of Action ◽

Kinase Inhibitor ◽

Clinical Development ◽

011 Preclinical Mechanism of Action of PRN1008, a Reversible Covalent Bruton’s Tyrosine Kinase Inhibitor in Clinical Development for Pemphigus

Journal of Investigative Dermatology ◽

10.1016/j.jid.2019.07.014 ◽

2019 ◽

Vol 139 (9) ◽

pp. S216

Author(s):

C.L. Langrish ◽

M.R. Francesco ◽

Y. Xing ◽

J.M. Bradshaw ◽

T.D. Owens ◽

...

Keyword(s):

Tyrosine Kinase ◽

Mechanism Of Action ◽

Kinase Inhibitor ◽

Clinical Development ◽

Phase I, first-in-human trial of Bruton’s tyrosine kinase inhibitor M7583 in patients with B-cell malignancies

Leukemia & Lymphoma ◽

10.1080/10428194.2021.1913139 ◽

2021 ◽

pp. 1-8

Author(s):

Wojciech Jurczak ◽

Simon Rule ◽

William Townsend ◽

David Tucker ◽

Barbara Sarholz ◽

...

Keyword(s):

Tyrosine Kinase ◽

Phase I ◽

B Cell ◽

Kinase Inhibitor ◽

B Cell Malignancies ◽

Human Trial

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 of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b00167 ◽

2019 ◽

Vol 62 (7) ◽

pp. 3228-3250 ◽

Cited By ~ 13

Author(s):

Scott H. Watterson ◽

Qingjie Liu ◽

Myra Beaudoin Bertrand ◽

Douglas G. Batt ◽

Ling Li ◽

...

Keyword(s):

Tyrosine Kinase ◽

Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.8b00461 ◽

2018 ◽

Vol 10 (1) ◽

pp. 80-85 ◽

Cited By ~ 2

Author(s):

Mark E. Schnute ◽

Stephen E. Benoit ◽

Ingrid P. Buchler ◽

Nicole Caspers ◽

Margaret L. Grapperhaus ◽

...

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Reactive Group ◽