The Development of BTK Inhibitors: A Five-Year Update
网页2021年12月6日 · The most active reported derivative (compound 1, Figure 5) inhibits BTKs at low nanomolar concentrations (IC 50 = 0.82 nM), suppress B-cell leukemia proliferations (Ramos and Raji cell lines) at concentrations of 3.17 mM and 6.69 mM, respectively, and blocks cell apoptosis, representing a promising BTK inhibitor for the treatment of B-cell ...
BTK Inhibitors: present and future - PMC - National Center for ...
网页BTK inhibitors, especially ibrutinib, have revolutionized the therapy of CLL, MCL and other B cell malignancies over the past few years, which is based on higher efficacy in patients with high-risk disease features, and better tolerability in elderly and frail patients when compared to CIT.
Inhibitors targeting Bruton’s tyrosine kinase in cancers: drug ...
网页2020年10月29日 · The Bruton tyrosine kinase (BTK) inhibitor PCI-32765 synergistically increases proteasome inhibitor activity in diffuse large-B cell lymphoma (DLBCL) and mantle cell lymphoma...
BTK inhibitors: past, present, and future - ScienceDirect
网页2024年8月1日 · Bruton’s tyrosine kinase (BTK) inhibitors have revolutionized the treatment landscape for B cell lymphomas such as chronic lymphocytic leukemia (CLL). The first-in-class BTK inhibitor ibrutinib has recently been succeeded by covalent BTK inhibitors that are safer but still face challenges of resistance mutations.
BTK inhibitors: past, present, and future - PubMed
网页Bruton's tyrosine kinase (BTK) inhibitors have revolutionized the treatment landscape for B cell lymphomas such as chronic lymphocytic leukemia (CLL). The first-in-class BTK inhibitor ibrutinib has recently been succeeded by covalent BTK inhibitors that are safer but still face challenges of resista ….
Second-Generation Bruton's Tyrosine Kinase Inhibitors: Simply …
网页2021年7月26日 · Acalabrutinib is an oral covalently binding BTK inhibitor that is approved by the US Food and Drug Administration (FDA) for marketing in the treatment of CLL.
Zanubrutinib: past, present, and future | Blood Cancer Journal
网页2023年9月11日 · Ibrutinib was the first BTK inhibitor to be approved, and it changed the standard-of-care treatment for diseases such as chronic lymphocytic leukemia, mantle cell lymphoma,...
Unlocking potential inhibitors for Bruton's tyrosine kinase
网页2023年10月17日 · Molecular docking-based virtual screening approach identified several repurposed drugs as potential BTK inhibitors, including Eltrombopag and Alectinib, which have already been approved for human...
Bruton’s Tyrosine Kinase Inhibitors: A New Generation of …
网页2021年9月27日 · BTK inhibitors may be a non-cell-depleting alternative to B cell modulation. In this review, the structure, signaling, and roles of BTK are reviewed among the different inhibitors assayed in animal models of MS and clinical trials.
Bruton Tyrosine Kinase Inhibitors: Present and Future
网页Bruton tyrosine kinase inhibitors are particularly active in patients with CLL and MCL, but also received approval for Waldenström macroglobulinemia, small lymphocytic lymphoma, marginal zone lymphoma, and chronic graft-versus-host disease.