Bruton's tyrosine kinase inhibitors in B-cell non-Hodgkin's lymphomas

2015 ◽  
Vol 97 (5) ◽  
pp. 469-477 ◽  
Author(s):  
L Alinari ◽  
C Quinion ◽  
KA Blum
Keyword(s):  
Tyrosine Kinase ◽  
B Cell ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase ◽  
Hodgkin's Lymphomas

Resistance to Bruton's Tyrosine Kinase Inhibitors: The Achilles Heel of Their Success Story in Lymphoid Malignancies

Blood ◽  
2021 ◽  
Author(s):  
Deborah M. Stephens ◽  
John C Byrd
Keyword(s):  
Tyrosine Kinase ◽  
B Cell ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Lymphocytic Leukemia ◽  
Treatment Modalities ◽  
Bruton’S Tyrosine Kinase ◽  
B Cell Malignancies ◽  
Bruton's Tyrosine Kinase ◽  
Resistant Disease

Bruton's tyrosine kinase inhibitors (BTKi) have significantly changed the treatment landscape for patients with B-cell malignancies including chronic lymphocytic leukemia (CLL), Waldenstrom's macroglobulinemia (WM), mantle cell lymphoma (MCL), and marginal zone lymphoma (MZL). Unfortunately, patients with BTKi resistant disease have shortened survival. Clinical and molecular risk factors, such as number of prior therapies and presence of TP53 mutations, can be used to predict patients at the highest risk of developing BTKi resistance. Many mechanisms of BTKi resistance have been reported with mutations in BTK and phospholipase C g 2 supported with the most data. The introduction of venetoclax has lengthened the survival of patients with BTKi resistant disease. Ongoing clinical trials with promising treatment modalities such as next-generation BTKi and chimeric antigen receptor T-cell therapy have reported promising efficacy in patients with BTKi resistant disease. Continued research focusing on resistance mechanisms and methods of how to circumvent resistance is needed to further prolong the survival of patients with BTKi resistant B-cell malignancies.

scholarly journals Discovery of new BTK inhibitors with B cell suppression activity bearing a 4,6-substituted thieno[3,2-d]pyrimidine scaffold

RSC Advances ◽  
2017 ◽  
Vol 7 (42) ◽  
pp. 26060-26069 ◽  
Author(s):  
Qiumeng Zhang ◽  
Luyao Zhang ◽  
Jie Yu ◽  
Heng Li ◽  
Shijun He ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
B Cell ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Bruton’S Tyrosine Kinase ◽  
Immunosuppressive Activity ◽  
Bruton's Tyrosine Kinase ◽  
Low Toxicity ◽  
Cell Suppression ◽  
Btk Inhibitors

Seventeen compounds with 4,6-substituted thieno[3,2-d]pyrimidine scaffold were prepared as new Bruton's tyrosine kinase inhibitors. Compound 8 exhibits anti-BTK activity, immunosuppressive activity, enzymatic selectivity and low toxicity.

scholarly journals Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors

MedChemComm ◽  
2018 ◽  
Vol 9 (4) ◽  
pp. 697-704 ◽  
Author(s):  
Haiyang Chen ◽  
Peiran Song ◽  
Yanyan Diao ◽  
Yongjia Hao ◽  
Dou Dou ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Enzymatic Activity ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase

Compound6potently inhibited the enzymatic activity of BTK with an IC50value of 1.9 nM.

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