BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies

A Alu, H Lei, X Han, Y Wei, X Wei - Journal of Hematology & Oncology, 2022 - Springer
Bruton's tyrosine kinase (BTK) is an essential component of multiple signaling pathways that
regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising …

Inhibitors targeting Bruton's tyrosine kinase in cancers: drug development advances

T Wen, J Wang, Y Shi, H Qian, P Liu - Leukemia, 2021 - nature.com
Bruton's tyrosine kinase (BTK) inhibitor is a promising novel agent that has potential
efficiency in B-cell malignancies. It took approximately 20 years from target discovery to new …

Long-term outcomes for ibrutinib–rituximab and chemoimmunotherapy in CLL: updated results of the E1912 trial

TD Shanafelt, XV Wang, CA Hanson… - Blood, The Journal …, 2022 - ashpublications.org
Herein, we present the long-term follow-up of the randomized E1912 trial comparing the
long-term efficacy of ibrutinib–rituximab (IR) therapy to fludarabine, cyclophosphamide, and …

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 …

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 …

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 …

Venetoclax in relapsed or refractory chronic lymphocytic leukaemia with 17p deletion: a multicentre, open-label, phase 2 study

S Stilgenbauer, B Eichhorst, J Schetelig… - The lancet …, 2016 - thelancet.com
Background Deletion of chromosome 17p (del [17p]) in patients with chronic lymphocytic
leukaemia confers very poor prognosis when treated with standard chemo-immunotherapy …

Targeting B cell receptor signalling in cancer: preclinical and clinical advances

JA Burger, A Wiestner - Nature Reviews Cancer, 2018 - nature.com
B cell receptor (BCR) signalling is crucial for normal B cell development and adaptive
immunity. BCR signalling also supports the survival and growth of malignant B cells in …

Long-term remissions after FCR chemoimmunotherapy in previously untreated patients with CLL: updated results of the CLL8 trial

K Fischer, J Bahlo, AM Fink, V Goede… - Blood, The Journal …, 2016 - ashpublications.org
Despite promising results with targeted drugs, chemoimmunotherapy with fludarabine,
cyclophosphamide (FC), and rituximab (R) remains the standard therapy for fit patients with …

Chronic lymphocytic leukaemia: from genetics to treatment

F Bosch, R Dalla-Favera - Nature reviews Clinical oncology, 2019 - nature.com
Chronic lymphocytic leukaemia (CLL), the most frequent type of leukaemia in adults, is a
lymphoproliferative disorder that is characterized by the expansion of monoclonal, mature …