Potent efficacy of MCL-1 inhibitor-based therapies in preclinical ...
WEBNov 26, 2019 — Ibrutinib reduced MCL-1 levels in Mino and Jeko1, and BCL-X L in Mino and Rec1 cells, whereas BCL-2 and BCL-W levels changed very little in all three lines (Fig. 3b).
Ibrutinib as Initial Therapy for Patients with Chronic Lymphocytic ...
WEBDec 17, 2015 — Ibrutinib is a first-in-class oral covalent inhibitor of Bruton’s tyrosine kinase (BTK) that has been approved for the treatment of patients with CLL who have received at least one prior...
Discovery of a highly potent and selective Bruton’s tyrosine kinase ...
WEBSep 14, 2020 — Ibrutinib, the first approved BTK inhibitor that binds irreversibly to cysteine residue 481, has shown potent clinical activity in the majority of CD20 positive B-cell malignancies. 2 However,...
Distinct BTK inhibitors differentially induce apoptosis but similarly ...
WEBJun 26, 2021 — Acalabrutinib and Zanubrutinib induced moderate apoptosis in Ibrutinib high-sensitive JeKo-1 cells and Ibrutinib low-sensitive Mino cells, which was accompanied by cleaved PARP and caspase-3.
Potentiation of apoptosis in drug-resistant mantle cell lymphoma …
WEBNov 2, 2023 — MCL cell lines that were sensitive or resistant to ibrutinib or venetoclax demonstrated susceptibility to AZD5991 (n = 9, IC 50 = 69.3 − 523.5 nM), and Mino exhibited a particularly high ...
Pirtobrutinib Overcomes Ibrutinib, Venetoclax Resistance in
WEBDec 12, 2021 — Pirtobrutinib (LOXO-305) was found to overcome both ibrutinib (Imbruvica) and venetoclax (Venclexta) resistance in heavily pretreated mantle cell lymphoma cells (MCL) cells, both in vitro and in...
Pirtobrutinib Overcomes Ibrutinib and Venetoclax Resistance in …
WEBNov 5, 2021 — Pirtobrutinib overcame both ibrutinib and venetoclax resistance in MCL cells in vitro and in vivo. G2/M checkpoints and E2F targets pathways were significantly enriched in both cases. Pirtobrutinib & venetoclax showed better in vivo efficacy in MCL models than combination of ibrutinib & venetoclax.
Ibrutinib–Rituximab or Chemoimmunotherapy for Chronic Lymphocytic ...
WEBJul 31, 2019 — The ibrutinib–rituximab regimen resulted in progression-free survival and overall survival that were superior to those with a standard chemoimmunotherapy regimen among patients 70 years of age...
Previously Treated MCL Resistant to Ibrutinib and Venetoclax …
WEBDec 12, 2021 — Treatment for 72 hours with dimethyl sulfoxide (DMSO), ibrutinib, and pirtobrutinib at a dosage of 10μM demonstrated that pirtobrutinib induced only marginal cell growth. Researchers used trypan blue exclusion assay to measure treatment objectives in cell lines 24, 48, and 72 hours following treatment with the agents.
Pirtobrutinib and venetoclax combination overcomes resistance to ...
WEBJeKo-ibrutinib (IBN)-R, Mino-venetoclax-R, Rec-venetoclax-R and Granta-519-venetoclax-R were generated by culturing parental cells with progressively increasing concentrations of ibrutinib or venetoclax.