BTK

Absorption, Metabolism, and Excretion of [14C]-Tolebrutinib After Oral Administration in Humans, Contribution of the Metabolites to Pharmacological Activity

22 views | Jan 23 2024

The study on tolebrutinib revealed extensive metabolism generating multiple metabolites, among which metabolite M2, constituting 4% of circulating radioactivity, retained potent inhibition of Bruton's tyrosine kinase akin to the parent compound, suggesting its likely contribution to the drug's pharmacological activity in vivo. [Read the Full Post]

A pilot study of orelabrutinib treatment in three cases of refractory/relapsed autoimmune haemolytic anaemia/Evans syndrome

42 views | Jan 07 2024

The promising response of nine out of twelve patients in our orelabrutinib trial for refractory/relapsed AIHA/Evans Syndrome indicates its potential as a new second-line treatment, offering hope for improved management and quality of life in these conditions. [Read the Full Post]

Assessment of the effects of Syk and BTK inhibitors on GPVI-mediated platelet signaling and function

0 views | Dec 17 2023

The study shows that small molecule tyrosine kinase inhibitors targeting Syk and BTK effectively inhibit essential platelet functions, such as adhesion, secretion, and aggregation, but exhibit differential effects on downstream signaling pathways and protein activities in platelets. [Read the Full Post]

Next-Generation Sequencing-Optimal Sequencing of Therapies in Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL)

0 views | Dec 04 2023

**This research paper provides a comprehensive overview of evidence-based sequencing of therapies in relapsed/refractory chronic lymphocytic leukemia (CLL) in the era of targeted drugs, emphasizing the importance of personalized treatment strategies and highlighting promising developments, such as noncovalent BTK inhibitors, while underscoring the urgent need for solutions in the challenging subgroup of patients previously exposed to both BTK and BCL2 inhibitors.** [Read the Full Post]

Antifibrotic mechanism of avitinib in bleomycin-induced pulmonary fibrosis in mice

22 views | Dec 01 2023

A new study demonstrates that avitinib attenuates bleomycin-induced pulmonary fibrosis in mice by inhibiting alveolar epithelial cell injury and myofibroblast activation, indicating its potential as a therapeutic option for this condition. [Read the Full Post]

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

27 views | Oct 17 2023

Fenebrutinib, an orally available Bruton tyrosine kinase inhibitor, has been characterized through in silico and in vitro studies, elucidating its metabolites and reactive intermediates, which can aid in understanding its adverse effects and facilitate the development of safer drugs. [Read the Full Post]

Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL)

0 views | Oct 02 2023

This review discusses the concept of relapsed chronic lymphocytic leukemia (CLL), available treatment options, and emerging therapies, emphasizing the need for individualized therapy selection and the ongoing research in this field. [Read the Full Post]

Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL)

25 views | Sep 30 2023

This review examines the recent advancements in the treatment of relapsed/refractory chronic lymphocytic leukemia (CLL), including targeted therapies, chimeric antigen receptor (CAR) T cell therapy, and the role of measurable residual disease (MRD) assessment, providing insights into therapeutic options and considerations for individualized treatment selection. [Read the Full Post]

Synthesis and Preclinical Evaluation of a Novel Fluorine-18-Labeled Tracer for Positron Emission Tomography Imaging of Bruton's Tyrosine Kinase

44 views | Sep 18 2023

[18F]PTBTK3, a PET radiotracer based on a selective BTK inhibitor, demonstrates BTK-dependent tumor uptake in BTK-positive tumors, showing promise for the diagnosis and development of BTK-targeted therapies. [Read the Full Post]

Remibrutinib inhibits hives effector cells stimulated by serum from chronic urticaria patients independently of FcεR1 expression level and omalizumab clinical response

71 views | Sep 18 2023

Remibrutinib, a Bruton's tyrosine kinase (BTK) inhibitor, effectively inhibits the activation of basophils and mast cells induced by serum from chronic urticaria patients, regardless of their responsiveness to omalizumab treatment. [Read the Full Post]