Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
In addition, compound 13e showed greater BTK selectivity and higher stability in human liver microsomes than IBN and potential safety improvement for the treatment of MCL.
|
31685258 |
2020 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
However, none of the treatment schedules containing BTK inhibitors have been shown to be curative in MCL.
|
31738609 |
2020 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Differential effects of BTK inhibitors ibrutinib and zanubrutinib on NK cell effector function in patients with mantle cell lymphoma.
|
31171645 |
2020 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Acalabrutinib is a novel second-generation oral Bruton tyrosine kinase inhibitor approved by the US Food and Drug Administration for relapsed MCL based on a clinical trial demonstrating an overall response rate of 81%.
|
30967367 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The dysregulation of PI3K signaling has been implicated as an underlying mechanism associated with resistance to Bruton's tyrosine kinase inhibition by ibrutinib in both chronic lymphocytic leukemia and mantle cell lymphoma (MCL).
|
30361685 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
We performed genomic, metabolomic, and fluxomic analyses to evaluate the mechanism of action of the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib (IBR) in mantle cell lymphoma (MCL) cells.
|
30862686 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Our studies suggest a general efficacy of BTK inhibition in MCL and potential drug resistance mechanism via alternative signaling pathways.
|
30413649 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Newer and more selective BTK inhibitors are currently in clinical development, including acalabrutinib, which is currently US FDA approved for previously treated mantle cell lymphoma.
|
30927175 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
We investigated a next-generation phosphoinositide-3-kinase-δ inhibitor (PI3K-δi), umbralisib, plus a Bruton tyrosine kinase inhibitor (BTKi), ibrutinib, in relapsed or refractory chronic lymphocytic leukaemia and mantle cell lymphoma.
|
30558987 |
2019 |
Mantle cell lymphoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Inhibitors of Bruton tyrosine kinase (BTK), a kinase downstream of BCR, display remarkable activity in a subset of mantle cell lymphoma (MCL) patients, but the drug resistance remains a considerable challenge.
|
31534006 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Moreover, we discovered DD-03-171, an optimized lead compound that exhibits enhanced antiproliferative effects on mantle cell lymphoma (MCL) cells in vitro by degrading BTK, IKFZ1, and IKFZ3 as well as efficacy against patient-derived xenografts in vivo.
|
30545835 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The introduction of inhibitors of Bruton's tyrosine kinase (BTK) into targeted therapy for MCL has significantly improved outcomes in patients with relapsed/refractory (R/R) disease.
|
31686856 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
USFDA has approved a novel Bruton tyrosine kinase (BTK) inhibitor acalabrutinib (ACA) for the treatment of mantle cell lymphoma in adults.
|
30453157 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib is a small molecule drug that targets Bruton's tyrosine kinase in B-cell malignancies and is highly efficient at killing mantle cell lymphoma and chronic lymphocytic leukemia.
|
30663221 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
We next demonstrated that BTK inhibition abrogated CSF1 and IL-10 production in MCL cells, leading to the inhibition of macrophage polarization and consequently resulting in the suppression of microenvironment-dependent MCL expansion.
|
30940906 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib, a BTK inhibitor, has demonstrated marked efficacy and tolerability in treatment-naïve, relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) and mantle cell lymphoma (MCL).
|
31638169 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Notably, 12a showed higher selectivity against BTK and exhibited robust antiproliferative effects in both mantle cell lymphoma cell lines and primary patient tumor cells.
|
31031018 |
2019 |
Mantle cell lymphoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
It has been proven that Bruton's tyrosine kinase (BTK) is commonly overexpressed in MCL, which makes it a focus of targeted therapy for MCL.
|
30857748 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Although intensive chemoimmunotherapy regimens that incorporate high-dose cytarabine and stem cell transplantation have improved survival in young and fit MCL patients, the introduction of Bruton tyrosine kinase inhibitors and other novel agents has made effective outpatient-based treatment accessible to nearly all MCL patients.
|
31808882 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib, a drug that inhibits Bruton's tyrosine kinase (BTK), has improved the overall survival of patients with MCL; however, resistance to ibrutinib has emerged as a decisive, negative factor in the prognosis of MCL.
|
30723172 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Expert commentary: Acalabrutinib, a new BTK inhibitor, currently being evaluated in numerous clinical studies is approved by FDA in relapsing/refractory MCL.
|
30638402 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Through genomic analyses of clinical specimens, we show that metabolic reprogramming toward oxidative phosphorylation (OXPHOS) and glutaminolysis is associated with therapeutic resistance to the Bruton's tyrosine kinase inhibitor ibrutinib in mantle cell lymphoma (MCL), a B cell lymphoma subtype with poor clinical outcomes.
|
31068440 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
In 2013, ibrutinib was approved by the FDA as the first-in-class BTK inhibitors for the treatment of mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL), and now it is also undergoing clinical evaluation for other indications in either single or combined therapy.
|
30888232 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
We previously demonstrated that prolonged early G1 cell cycle arrest induced by the oral, specific CDK4/6 inhibitor palbociclib can overcome ibrutinib resistance in primary human MCL cells and MCL cell lines expressing wild-type Bruton's tyrosine kinase (BTK).
|
30692121 |
2019 |
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The BTK inhibitor ibrutinib has been approved as a therapy for refractory MCL, and while it shows some clinical activity, patients frequently develop primary or secondary ibrutinib resistance and have very poor outcomes after relapsing following ibrutinib treatment.
|
29441438 |
2018 |