Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia

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Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia is …
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scholarly articleQ13442814

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P356DOI10.1158/1078-0432.CCR-14-2809
P932PMC publication ID4537801
P698PubMed publication ID25829398

P50authorWilliam G WierdaQ64026278
Michael J. KeatingQ66429598
Jennifer A WoyachQ90156409
Kumudha BalakrishnanQ114427990
Fabiola Cervantes-GomezQ117256519
Betty LamotheQ117256520
P2093author name stringVarsha Gandhi
P2860cites workThe Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancyQ24633214
Bcl-2 antagonists: a proof of concept for CLL therapyQ26823996
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing plateletsQ27683708
Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinibQ27853011
Chronic lymphocytic leukemiaQ28236621
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High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cellsQ30433183
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MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignanciesQ33419789
Ibrutinib inhibits BCR and NF-κB signaling and reduces tumor proliferation in tissue-resident cells of patients with CLLQ33714712
Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignanciesQ33893704
Discovery of selective irreversible inhibitors for Bruton's tyrosine kinaseQ34001339
Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765.Q34026194
The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivoQ34029869
Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signalsQ34184717
Safety and activity of ibrutinib plus rituximab for patients with high-risk chronic lymphocytic leukaemia: a single-arm, phase 2 studyQ34240404
The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemiaQ34249777
Long-term results of first salvage treatment in CLL patients treated initially with FCR (fludarabine, cyclophosphamide, rituximab)Q34508322
The lymph node microenvironment promotes B-cell receptor signaling, NF-κB activation, and tumor proliferation in chronic lymphocytic leukemiaQ34542102
Regulation of Mcl-1 expression in context to bone marrow stromal microenvironment in chronic lymphocytic leukemiaQ35022490
Chronic lymphocytic leukemia requires BCL2 to sequester prodeath BIM, explaining sensitivity to BCL2 antagonist ABT-737.Q35250940
How I treat refractory CLL.Q36276536
Autoantigen can promote progression to a more aggressive TCL1 leukemia by selecting variants with enhanced B-cell receptor signalingQ36782109
Bendamustine in B-Cell Malignancies: The New 46-Year-Old Kid on the BlockQ37480786
Long-term results of the fludarabine, cyclophosphamide, and rituximab regimen as initial therapy of chronic lymphocytic leukemiaQ37634897
From pathogenesis to treatment of chronic lymphocytic leukaemiaQ37643423
Prolonged lymphocytosis during ibrutinib therapy is associated with distinct molecular characteristics and does not indicate a suboptimal response to therapyQ37655012
Inhibiting B-cell receptor signaling pathways in chronic lymphocytic leukemiaQ37959298
Targeting the microenvironment in chronic lymphocytic leukemia is changing the therapeutic landscapeQ38041898
"Role of the B-cell receptor and the microenvironment in chronic lymphocytic leukemia''.Q38140625
Lymph node-induced immune tolerance in chronic lymphocytic leukaemia: a role for caveolin-1.Q38325527
First-line therapy with fludarabine compared with chlorambucil does not result in a major benefit for elderly patients with advanced chronic lymphocytic leukemiaQ38380183
Functional characterization of BTK(C481S) mutation that confers ibrutinib resistance: exploration of alternative kinase inhibitors.Q38959765
BTK inhibition targets in vivo CLL proliferation through its effects on B-cell receptor signaling activityQ39056302
The Akt/Mcl-1 pathway plays a prominent role in mediating antiapoptotic signals downstream of the B-cell receptor in chronic lymphocytic leukemia B cellsQ40069478
Sustained signaling through the B-cell receptor induces Mcl-1 and promotes survival of chronic lymphocytic leukemia B cells.Q40455255
High-level expression of the T-cell chemokines CCL3 and CCL4 by chronic lymphocytic leukemia B cells in nurselike cell cocultures and after BCR stimulationQ42184742
PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease modelsQ42708522
Proteasome inhibitor carfilzomib complements ibrutinib's action in chronic lymphocytic leukemiaQ43096794
Chemoimmunotherapy with fludarabine, cyclophosphamide, and rituximab for relapsed and refractory chronic lymphocytic leukemiaQ46378902
Gene mutations and treatment outcome in chronic lymphocytic leukemia: results from the CLL8 trial.Q53061290
Combination of ibrutinib with ABT-199: synergistic effects on proliferation inhibition and apoptosis in mantle cell lymphoma cells through perturbation of BTK, AKT and BCL2 pathways.Q55070853
The BCL2 antagonist ABT-199 triggers apoptosis, and augments ibrutinib and idelalisib mediated cytotoxicity in CXCR4 Wild-type and CXCR4 WHIM mutated Waldenstrom macroglobulinaemia cellsQ86516013
P433issue16
P407language of work or nameEnglishQ1860
P921main subjectleukemiaQ29496
ibrutinibQ5984881
lymphocyteQ715347
chronic lymphocytic leukemiaQ1088156
venetoclaxQ23671272
P304page(s)3705-3715
P577publication date2015-03-31
P1433published inClinical Cancer ResearchQ332253
P1476titlePharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia
P478volume21

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