Role of Bruton's tyrosine kinase in B cells and malignancies

S Pal Singh, F Dammeijer, RW Hendriks - Molecular cancer, 2018 - Springer
Bruton's tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic
signaling that is critical for proliferation and survival of leukemic cells in many B cell …

BCL2 and MCL1 inhibitors for hematologic malignancies

AW Roberts, AH Wei… - Blood, The Journal of the …, 2021 - ashpublications.org
BCL2 and MCL1 are commonly expressed prosurvival (antiapoptotic) proteins in
hematologic cancers and play important roles in their biology either through dysregulation or …

Long-term efficacy and safety of first-line ibrutinib treatment for patients with CLL/SLL: 5 years of follow-up from the phase 3 RESONATE-2 study

JA Burger, PM Barr, T Robak, C Owen, P Ghia… - Leukemia, 2020 - nature.com
RESONATE-2 is a phase 3 study of first-line ibrutinib versus chlorambucil in chronic
lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). Patients aged≥ 65 years …

Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL

CS Tam, J Trotman, S Opat, JA Burger… - Blood, The Journal …, 2019 - ashpublications.org
Zanubrutinib is a potent and highly selective inhibitor of Bruton tyrosine kinase (BTK). In this
first-in-human, open-label, multicenter, phase 1 study, patients in part 1 (3+ 3 dose …

Zanubrutinib in patients with previously treated B-cell malignancies intolerant of previous Bruton tyrosine kinase inhibitors in the USA: a phase 2, open-label, single …

M Shadman, IW Flinn, MY Levy, RF Porter… - The Lancet …, 2023 - thelancet.com
Background We hypothesised that zanubrutinib, a highly selective next-generation Bruton
tyrosine kinase (BTK) inhibitor, would be a safe and active treatment for patients intolerant of …

Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of Bruton's tyrosine kinase

Y Guo, YE Liu, N Hu, D Yu, C Zhou, G Shi… - Journal of Medicinal …, 2019 - ACS Publications
Aberrant activation of Bruton's tyrosine kinase (BTK) plays an important role in pathogenesis
of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of …

Comparative analysis of BTK inhibitors and mechanisms underlying adverse effects

HY Estupiñán, A Berglöf, R Zain… - Frontiers in cell and …, 2021 - frontiersin.org
The cytoplasmic protein-tyrosine kinase BTK plays an essential role for differentiation and
survival of B-lineage cells and, hence, represents a suitable drug target. The number of BTK …

Ibrutinib plus obinutuzumab versus chlorambucil plus obinutuzumab in first-line treatment of chronic lymphocytic leukaemia (iLLUMINATE): a multicentre, randomised …

C Moreno, R Greil, F Demirkan, A Tedeschi… - The Lancet …, 2019 - thelancet.com
Background Both single-agent ibrutinib and chlorambucil plus obinutuzumab have shown
superior efficacy to chlorambucil monotherapy and are standard first-line treatments in …

Targeting BCL2 with venetoclax in relapsed chronic lymphocytic leukemia

AW Roberts, MS Davids, JM Pagel… - … England Journal of …, 2016 - Mass Medical Soc
Background New treatments have improved outcomes for patients with relapsed chronic
lymphocytic leukemia (CLL), but complete remissions remain uncommon. Venetoclax has a …

The phase 3 DUO trial: duvelisib vs ofatumumab in relapsed and refractory CLL/SLL

IW Flinn, P Hillmen, M Montillo, Z Nagy… - Blood, The Journal …, 2018 - ashpublications.org
Duvelisib (also known as IPI-145) is an oral, dual inhibitor of phosphatidylinositol 3-kinase δ
and γ (PI3K-δ, γ) being developed for treatment of hematologic malignancies. PI3K-δ, γ …