Comparison of Intermolecular Interactions of Irreversible and Reversible Inhibitors with Bruton's Tyrosine Kinase via Molecular Dynamics Simulations - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36364276/
Bruton's tyrosine kinase (BTK) is a key protein from the TEC family and is involved in B-cell lymphoma occurrence and development. Targeting BTK is therefore an effective strategy for B-cell...
Conclusions: Our results provide mechanistic insights into resistance against BTK-targeting drugs and the key interaction sites for the development of high-quality BTK inhibitors. The steered dynamics simulation also offers a means to rapidly assess the binding capacity of newly designed inhibitors.
Ibrutinib and Bruton's tyrosine kinase inhibitors in chronic lymphocytic leukemia: focus on atrial fibrillation and ventricular tachyarrhythmias/sudden cardiac death - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36366814/
For this reason, caution should be exercised before concluding that second-generation BTK inhibitors are safer than ibrutinib. Recent data on the effectiveness of ibrutinib over a follow-up of 8 years...
Conclusions: Recent data on the effectiveness of ibrutinib over a follow-up of 8 years show a remarkable benefit on all-cause mortality, which is of great value also for interpreting the clinical impact of the few cases of VA and sudden cardiac death (SCD) reported for ibrutinib, independently of QT lengthening. Since a risk of VA and SCD has...
Evaluating orelabrutinib as a novel treatment option for relapsed/refractory chronic lymphocytic leukemia in China - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36329558/
Orelabrutinib selectively inhibits BTK via covalent binding and exhibits linear pharmacokinetics. BTK is the only kinase targeted by orelabrutinib, and a few off-target toxicities of orelabrutinib have been reported. The...
Expert Opinion: Orelabrutinib selectively inhibits BTK via covalent binding and exhibits linear pharmacokinetics. BTK is the only kinase targeted by orelabrutinib, and a few off-target toxicities of orelabrutinib have been reported. The phase I/II trial demonstrated the efficacy and safety of orelabrutinib in patients with R/R CLL/SLL; however,...
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Leukemia and Lymphoma Connect3yrKey Points • Source: Expert Opinion on Pharmacotherapy • Conclusions/Relevance: “Orelabrutinib selectively inhibits BTK via covalent binding and exhibits linear pharmacokinetics. BTK is the only kinase targeted by orelabrutinib, and a few off-target toxicities Show More
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Source : https://europepmc.org/article/med/36314537
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Conclusions/Relevance: We report the discovery and preclinical properties of JNJ-64264681 (13), a covalent, irreversible BTK inhibitor with potent whole blood activity and exceptional kinome selectivity. JNJ-64264681 demonstrated excellent oral efficacy in both cancer and autoimmune models with sustained in vivo target coverage amenable to once...
Topical Delivery of Bruton's Tyrosine Kinase (BTK) Inhibitor and Curcumin Loaded Nano-structured Lipid Carrier Gel: Repurposing Strategy for the Psoriasis Management - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36330998/
Current work investigates the synergistic potential of nanostructured lipid carrier (NLC) gel of Ibrutinib with Curcumin as repurposing strategy to treat psoriasis. In the present work, various components such as...
Conclusions: The study suggested integrated benefits of repurposing Ibrutinib with Curcumin as NLC topical gel and it could possibly reduce remission of Psoriasis like inflammation and merit additional investigation.