Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase

MS Davids, JR Brown - Future oncology, 2014 - Taylor & Francis
Ibrutinib (formerly PCI-32765) is a potent, covalent inhibitor of Bruton's tyrosine kinase, a
kinase downstream of the B-cell receptor that is critical for B-cell survival and proliferation. In …

Ibrutinib: first global approval

F Cameron, M Sanford - Drugs, 2014 - Springer
Ibrutinib (Imbruvica™) is a small molecule, first-in-class, once-daily, orally available, Bruton's
tyrosine kinase inhibitor that is under development for the treatment of B cell malignancies …

Somatic mutations in MYD88 and CXCR4 are determinants of clinical presentation and overall survival in Waldenström macroglobulinemia

SP Treon, Y Cao, L Xu, G Yang, X Liu… - Blood, The Journal of …, 2014 - ashpublications.org
Whole genome sequencing has revealed activating somatic mutations in MYD88 (L265P)
and CXCR4 in Waldenström macroglobulinemia (WM). CXCR4 somatic mutations in WM …

Partial reconstitution of humoral immunity and fewer infections in patients with chronic lymphocytic leukemia treated with ibrutinib

C Sun, X Tian, YS Lee, S Gunti, A Lipsky… - Blood, The Journal …, 2015 - ashpublications.org
Chronic lymphocytic leukemia (CLL) is characterized by immune dysregulation, often
including hypogammaglobulinemia, which contributes to a high rate of infections and …

The WHIM-like CXCR4S338X somatic mutation activates AKT and ERK, and promotes resistance to ibrutinib and other agents used in the treatment of Waldenstrom's …

Y Cao, ZR Hunter, X Liu, L Xu, G Yang, J Chen… - Leukemia, 2015 - nature.com
CXCR4 WHIM somatic mutations are common Waldenstrom's Macroglobulinemia (WM), and
are associated with clinical resistance to ibrutinib. We engineered WM cells to express the …

C1013G/CXCR4 acts as a driver mutation of tumor progression and modulator of drug resistance in lymphoplasmacytic lymphoma

AM Roccaro, A Sacco, C Jimenez… - Blood, The Journal …, 2014 - ashpublications.org
The CXC chemokine receptor type 4 (CXCR4) plays a crucial role in modulating cell
trafficking in hematopoietic stem cells and clonal B cells. We screened 418 patients with B …

Clonal evolution underlying leukemia progression and Richter transformation in patients with ibrutinib-relapsed CLL

S Kadri, J Lee, C Fitzpatrick, N Galanina… - Blood …, 2017 - ashpublications.org
Ibrutinib has generated remarkable responses in patients with chronic lymphocytic leukemia
(CLL), including those with an unfavorable cytogenetic profile. However, patients develop …

Carfilzomib, rituximab, and dexamethasone (CaRD) treatment offers a neuropathy-sparing approach for treating Waldenström's macroglobulinemia

SP Treon, CK Tripsas, K Meid, S Kanan… - Blood, The Journal …, 2014 - ashpublications.org
Bortezomib frequently produces severe treatment-related peripheral neuropathy (PN) in
Waldenström's macroglobulinemia (WM). Carfilzomib is a neuropathy-sparing proteasome …

Targeted therapies in CLL: mechanisms of resistance and strategies for management

JA Woyach, AJ Johnson - Blood, The Journal of the American …, 2015 - ashpublications.org
The therapy of relapsed chronic lymphocytic leukemia (CLL) has changed dramatically in
the past year with the regulatory approval of idelalisib and ibrutinib, with other therapeutic …

Overall survival and competing risks of death in patients with W aldenström macroglobulinaemia: an analysis of the S urveillance, E pidemiology and E nd R esults …

JJ Castillo, AJ Olszewski, S Kanan… - British Journal of …, 2015 - Wiley Online Library
Waldenström macroglobulinaemia (WM) is a rare and incurable lymphoma. Given that the
survival of WM patients can be prolonged, our objective was to describe trends in overall …