|
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 |
HSP90 inhibition induced the complete degradation of both BTK and IκB kinase α in MCL lines and CD40-dependent B cells, with downstream loss of MAPK and nonclassical NF-κB signaling.
|
27742706 |
2016 |
|
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 |
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 |
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 |
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 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Acquired resistance to cancer drugs is common, also for modern targeted drugs like the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, a new drug approved for the treatment of the highly aggressive and relapsing mantle cell lymphoma (MCL).
|
29483220 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Mantle cell lymphoma (MCL) is characterized by increased B-cell receptor (BCR) signaling, and BTK inhibition is an effective therapeutic intervention in MCL patients.
|
29615403 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib, a clinically approved irreversible BTK kinase inhibitor for Mantle Cell Lymphoma (MCL) and Chronic Lymphocytic Leukemia (CLL) etc, has been reported to be potent against EGFR mutant kinase and currently being evaluated in clinic for Non Small Cell Lung Cancer (NSCLC).
|
27626175 |
2016 |
|
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 |
Biomarker
|
disease |
BEFREE |
At the time of relapse, agents directed at activated pathways in MCL cells such as bortezomib (NFkB inhibitor), lenalidamide (anti-angiogenesis) and Ibruitinib (Bruton's Tyrosine Kinase [BTK] inhibitor) have demonstrated excellent clinical activity in MCL patients.
|
26103436 |
2015 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Several second generation BTK inhibitors are in clinical development and might further improve tolerability and efficacy of therapy in advanced stage CLL and MCL.
|
28661188 |
2017 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Despite the development of the novel Bruton tyrosine kinase inhibitor ibrutinib, mantle cell lymphoma (MCL) remains an incurable B-cell non-Hodgkin lymphoma.
|
29983879 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The Bruton tyrosine kinase (BTK) inhibitor, ibrutinib, has produced remarkable clinical response in chronic lymphocytic leukemia (CLL) and mantle cell lymphoma.
|
25189416 |
2015 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Inhibition of B-cell receptor (BCR) signaling through the BTK inhibitor, ibrutinib, has generated a remarkable response in mantle cell lymphoma (MCL).
|
30510142 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib is an orally bioavailable and highly specific BTK inhibitor that was recently approved for treatment of patients with recurrent CLL and mantle cell lymphoma (MCL).
|
25858358 |
2015 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib, an oral Bruton tyrosine kinase inhibitor, has demonstrated efficacy and CNS penetration in relapsed or refractory MCL with rapid and complete response even after 1 year of follow-up.
|
28063897 |
2017 |
|
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 |
We have discovered the first relapse-specific BTK mutation in patients with MCL with acquired resistance, but not primary resistance, to ibrutinib, and demonstrated a rationale for targeting the proliferative resistant MCL cells by inhibiting CDK4 and the cell cycle in combination with ibrutinib in the presence of BTK(WT) or a PI3K inhibitor independent of BTK mutation.
|
25082755 |
2014 |
|
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 |
Interestingly, targeting BTK and SYK prevented and inhibited BCR-induced MCL cell adhesion to human bone marrow stromal cells (HMSCs) in short- and long-term co-culture.
|
25388373 |
2015 |
|
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 |
Furthermore, α-BCR-induced signaling strength was variable across patient samples and correlated with BCR subunit CD79B expression, but was inversely correlated with susceptibility to Bruton tyrosine kinase (BTK) and SYK inhibitors in MCL.
|
28011673 |
2017 |