|
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), BTK inhibitors or CAL-101 (B-cell receptor inhibitors) or lenalidamide (antiangiogenesis) have clinical activity in MCL patients.
|
22615102 |
2012 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Treatment of MCL cell lines (Mino or Jeko-1) with a potent BTK pharmacologic inhibitor, Ibrutinib, decreased phospho-BTK-Tyr(223) expression.
|
23962569 |
2013 |
|
Mantle cell lymphoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Clinical trials with Ibruitinib (Bruton's Tyrosine Kinase inhibitor) or Idelalisib (PI3K inhibitor) have demonstrated excellent clinical activity in MCL patients.
|
24273091 |
2013 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib (PCI-32765) is the most advanced BTK inhibitor in clinical testing, with ongoing phase III clinical trials in patients with chronic lymphocytic leukemia and mantle-cell lymphoma.
|
24778403 |
2014 |
|
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 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 |
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 |
Biological rational for sequential targeting of Bruton tyrosine kinase and Bcl-2 to overcome CD40-induced ABT-199 resistance in mantle cell lymphoma.
|
25797245 |
2015 |
|
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 |
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 |
Strong synergism was observed with pimasertib combined with the PI3K inhibitor idelalisib and the BTK inhibitor ibrutinib in cell lines derived from diffuse large B-cell lymphoma (DLBCL) and mantle cell lymphoma.
|
26961147 |
2016 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Ibrutinib, a Bruton's tyrosine kinase inhibitor, is the newest drug in the arsenal that has shown promising efficacy in relapsed mantle cell lymphoma.
|
26970573 |
2017 |
|
Mantle cell lymphoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Recently, the Bruton tyrosine kinase (BTK) inhibitor ibrutinib demonstrated important clinical activity in MCL.
|
27127301 |
2016 |
|
Mantle cell lymphoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
FBXO10 deficiency and BTK activation upregulate BCL2 expression in mantle cell lymphoma.
|
27157620 |
2016 |
|
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 |
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 |
AlteredExpression
|
disease |
BEFREE |
Targeting the HDACs by using either RNA interference against HDAC1 in CLL or a small molecule inhibitor (HDACi) in CLL and mantle cell lymphoma restored the expression of the BTK-targeting miRs with loss of BTK protein and downstream signaling and consequent cell death.
|
27756747 |
2016 |
|
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 |
|
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 |
Two agents are already approved in the USA and Europe: ibrutinib, a BTK inhibitor, for the treatment of chronic lymphatic leukaemia (CLL), mantle cell lymphoma (MCL) and Waldenström's macroglobulinemia; and idelalisib, a PI3Kδ inhibitor, for the treatment of CLL and follicular lymphoma.
|
28295729 |
2017 |
|
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 |
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.
|
28699667 |
2017 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Taken together, simultaneous suppression of BTK and mTOR may be indicated as a potential therapeutic modality for the treatment of MCL.
|
28905990 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Bruton tyrosine kinase is a clinically validated target in mantle cell lymphoma.
|
29241979 |
2018 |
|
Mantle cell lymphoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Introduction of the Bruton tyrosine kinase (BTK) inhibitor ibrutinib has markedly improved MCL therapy outcome, but drug resistance remains a challenge.
|
29296874 |
2017 |