Comparative analysis of BTK inhibitors and mechanisms underlying adverse effects

HY Estupiñán, A Berglöf, R Zain… - Frontiers in cell and …, 2021 - frontiersin.org
The cytoplasmic protein-tyrosine kinase BTK plays an essential role for differentiation and
survival of B-lineage cells and, hence, represents a suitable drug target. The number of BTK …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

[HTML][HTML] Zanubrutinib or ibrutinib in relapsed or refractory chronic lymphocytic leukemia

JR Brown, B Eichhorst, P Hillmen… - … England Journal of …, 2023 - Mass Medical Soc
Background In a multinational, phase 3, head-to-head trial, ibrutinib, a Bruton's tyrosine
kinase (BTK) inhibitor, was compared with zanubrutinib, a BTK inhibitor with greater …

Phase I/II study of tirabrutinib, a second-generation Bruton's tyrosine kinase inhibitor, in relapsed/refractory primary central nervous system lymphoma

Y Narita, M Nagane, K Mishima, Y Terui… - Neuro …, 2021 - academic.oup.com
Background The safety, tolerability, efficacy, and pharmacokinetics of tirabrutinib, a second-
generation, highly selective oral Bruton's tyrosine kinase inhibitor, were evaluated for …

Zanubrutinib versus ibrutinib in relapsed/refractory chronic lymphocytic leukemia and small lymphocytic lymphoma: interim analysis of a randomized phase III trial

P Hillmen, B Eichhorst, JR Brown… - Journal of Clinical …, 2023 - ascopubs.org
PURPOSE Zanubrutinib is a potent, irreversible next-generation Bruton tyrosine kinase
(BTK) inhibitor designed to maximize BTK occupancy and minimize off-target kinase …

Cumulative incidence, risk factors, and management of atrial fibrillation in patients receiving ibrutinib

TE Wiczer, LB Levine, J Brumbaugh, J Coggins… - Blood …, 2017 - ashpublications.org
Atrial fibrillation (AF) has been reported in up to 16% of patients taking ibrutinib. Data
regarding the management of AF in this patient population are limited, and stroke prevention …

Clinical pharmacology and PK/PD translation of the second-generation Bruton's tyrosine kinase inhibitor, zanubrutinib

CS Tam, YC Ou, J Trotman, S Opat - Expert Review of Clinical …, 2021 - Taylor & Francis
Introduction: Bruton's tyrosine kinase (BTK) inhibitors have revolutionized the treatment of B-
cell lymphomas. Zanubrutinib was designed to achieve improved therapeutic concentrations …

A review of HER4 (ErbB4) kinase, its impact on cancer, and its inhibitors

MI El-Gamal, NH Mewafi, NE Abdelmotteleb… - Molecules, 2021 - mdpi.com
HER4 is a receptor tyrosine kinase that is required for the evolution of normal body systems
such as cardiovascular, nervous, and endocrine systems, especially the mammary glands. It …

DTI-HETA: prediction of drug–target interactions based on GCN and GAT on heterogeneous graph

K Shao, Y Zhang, Y Wen, Z Zhang… - Briefings in …, 2022 - academic.oup.com
Drug–target interaction (DTI) prediction plays an important role in drug repositioning, drug
discovery and drug design. However, due to the large size of the chemical and genomic …

Ibrutinib combinations in CLL therapy: scientific rationale and clinical results

N Timofeeva, V Gandhi - Blood cancer journal, 2021 - nature.com
Ibrutinib has revolutionized the treatment of chronic lymphocytic leukemia (CLL). This drug
irreversibly inhibits Bruton tyrosine kinase (BTK) by covalently binding to the C481 residue …