Results 1 to 10 of about 580 (130)

A Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Fenebrutinib and Effect on the QT/QTc Interval in Healthy Participants [PDF]

Clinical and Translational Science
Fenebrutinib is a Bruton's tyrosine kinase inhibitor under investigation for the treatment of multiple sclerosis. The goal of this study was to investigate the effect of fenebrutinib on cardiac repolarization (QT interval) as well as its safety ...
Yan Xu, Sonoko Kawakatsu, Denison Kuruvilla, John N. Ratchford, Qi Qi, Malgorzata Sierzega, Lin Pan, Jiajie Yu   +7 more
doaj   +6 more sources

Physiologically-Based Pharmacokinetic Model-Informed Drug Development for Fenebrutinib: Understanding Complex Drug-Drug Interactions [PDF]

CPT: Pharmacometrics and Systems Pharmacology, 2020
Fenebrutinib is a CYP3A substrate and time‐dependent inhibitor, as well as a BCRP and OATP1B transporter inhibitor in vitro. Physiologically‐based pharmacokinetic (PBPK) modeling strategies with the ultimate goal of understanding complex drug‐drug ...
Yuan Chen, Matthew Wright, Leslie W Chinn   +2 more
exaly   +5 more sources

Development of a Fast and Sensitive UPLC–MS/MS Analytical Methodology for Fenebrutinib Estimation in Human Liver Microsomes: In Vitro and In Silico Metabolic Stability Evaluation

Separations, 2023
Fenebrutinib (GDC-0853; FNB) is an oral small molecule that was developed by Roche Pharmaceuticals to slow multiple sclerosis progression. FNB is a reversible bruton tyrosine kinase (BTK) inhibitor, which showed the maximum potency of BTK inhibitors in ...
Adnan Kadı, Haya aljohar, Mohamed W Attwa   +2 more
exaly   +5 more sources

Investigation of Fenebrutinib Metabolism and Bioactivation Using MS³ Methodology in Ion Trap LC/MS

Molecules, 2023
Fenebrutinib is an orally available Bruton tyrosine kinase inhibitor. It is currently in multiple phase III clinical trials for the management of B-cell tumors and autoimmune disorders.
Aishah M. Alsibaee, Haya I. Aljohar, Mohamed W. Attwa, Ali S. Abdelhameed, Adnan A. Kadi   +4 more
doaj   +4 more sources

Fenebrutinib, a Bruton’s tyrosine kinase inhibitor, blocks distinct human microglial signaling pathways [PDF]

Journal of Neuroinflammation
Background Bruton’s tyrosine kinase (BTK) is an intracellular signaling enzyme that regulates B-lymphocyte and myeloid cell functions. Due to its involvement in both innate and adaptive immune compartments, BTK inhibitors have emerged as a therapeutic ...
Julie Langlois, Simona Lange, Martin Ebeling, Will Macnair, Roland Schmucki, Cenxiao Li, Jonathan DeGeer, Tania J. J. Sudharshan, V. Wee Yong, Yun-An Shen, Christopher Harp, Ludovic Collin, James Keaney   +12 more
doaj   +5 more sources

Biological and target synthetic treatments for chronic spontaneous urticaria: A systematic review and network meta‐analysis [PDF]

Clinical and Translational Allergy
Background Most biological and synthetic target‐specific drugs for antihistamine‐refractory chronic spontaneous urticaria (CSU) have not been compared head‐to‐head.
Zuotao Zhao, Yaqi Zheng, Xiaoting Song, Chengyue Peng, Shuanglu Liao, Peixin Zhang, Yen Tan, Xiaojie Huang, Litao Zhang   +8 more
doaj   +3 more sources

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

Frontiers in Immunology, 2021
Low-molecular weight chemical compounds have a longstanding history as drugs. Target specificity and binding efficiency represent major obstacles for small molecules to become clinically relevant. Protein kinases are attractive cellular targets; however,
Rula Zain, Rula Zain, Mauno Vihinen
doaj   +3 more sources

Bruton’s Tyrosine Kinase Inhibitors in Multiple Sclerosis: Mechanistic Considerations Across Relapsing and Progressive Disease [PDF]

Molecules
Multiple sclerosis (MS) reflects a dynamic interplay between peripheral immune activation and compartmentalized inflammation within the central nervous system (CNS).
Qiying Ye, Siming Ma
doaj   +2 more sources

Emerging Role of BTK Inhibitors in Multiple Sclerosis: From Immunobiology to Clinical Translation [PDF]

Brain Sciences
Background: Multiple sclerosis (MS), an autoimmune disease, involves peripheral immune activation followed by CNS inflammation in a compartmentalized manner.
Aashray Raj, Vansh Patel, Mehak Dang, Aken Kayastha, Yusuf Kagzi, Praveen Nandha Kumar Pitchan Velammal, Nidhi Agrawal, Kushagra Sharma, Nicholas Hansen, Sijin Wen, Shruti Jaiswal, Shitiz Sriwastava   +11 more
doaj   +2 more sources

Comparative CNS Pharmacology of the Bruton’s Tyrosine Kinase (BTK) Inhibitor Tolebrutinib Versus Other BTK Inhibitor Candidates for Treating Multiple Sclerosis [PDF]

Drugs in R&D
Background and objectives Tolebrutinib is a covalent BTK inhibitor designed and selected for potency and CNS exposure to optimize impact on BTK-dependent signaling in CNS-resident cells.
Timothy J. Turner, Pricilla Brun, Ross C. Gruber, Dimitry Ofengeim   +3 more
doaj   +2 more sources