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9d
Tirabrutinib-anthracycline interactions in the brain tumor microenvironment: a focus on metabolic inactivation and resistance. (PubMed, Expert Opin Drug Metab Toxicol)
Our in vitro data demonstrate that tirabrutinib influences daunorubicin pharmacodynamics by targeting both metabolic and transport pathways. However, Chou - Talalay analysis highlights the importance of appropriate dosing to achieve therapeutic synergy in combination regimens.
Journal
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AKR1C3 (Aldo-Keto Reductase Family 1 Member C3)
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daunorubicin • Velexbru (tirabrutinib)
1m
Bing-Neel Syndrome in Waldenström Macroglobulinemia: Updates on Clinical Management and BTK Inhibitor Efficacy. (PubMed, Cancers (Basel))
Historically, high-dose methotrexate- or cytarabine-based chemotherapy, intrathecal therapy, and radiotherapy have been used; however, responses varied, and toxicity was considerable...Retrospective data support durable responses with ibrutinib, tirabrutinib, and zanubrutinib, while early findings suggest that non-covalent BTK inhibitors expand options for relapsed or refractory cases. Herein, we synthesize current evidence on epidemiology, pathophysiology, and diagnostic work-up. We also outline therapeutic recommendations integrating the genotype, disease pattern, and patient fitness and conclude with unmet needs and future directions.
Review • Journal
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MYD88 (MYD88 Innate Immune Signal Transduction Adaptor)
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Imbruvica (ibrutinib) • cytarabine • Brukinsa (zanubrutinib) • methotrexate • Jaypirca (pirtobrutinib) • Velexbru (tirabrutinib) • methotrexate IV
1m
Study of Tirabrutinib (ONO-4059) in Patients With Primary Central Nervous System Lymphoma (PROSPECT Study) (clinicaltrials.gov)
P2, N=119, Active, not recruiting, Ono Pharmaceutical Co. Ltd | Recruiting --> Active, not recruiting
Enrollment closed
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temozolomide • Velexbru (tirabrutinib)
2ms
A Study to Investigate the Pharmacokinetics of Tirabrutinib in Participants With Mild, Moderate, and Severe Hepatic Impairment Compared to Healthy Participants (clinicaltrials.gov)
P1, N=32, Recruiting, Ono Pharmaceutical Co. Ltd | Not yet recruiting --> Recruiting | N=24 --> 32 | Initiation date: Jan 2026 --> Oct 2025
Enrollment open • Enrollment change • Trial initiation date
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Velexbru (tirabrutinib)
2ms
Membranous nephropathy preceding Bing-Neel syndrome: successful treatment with tirabrutinib. (PubMed, J Nephrol)
Despite initial partial remission with corticosteroids and cyclosporine, neurological symptoms emerged alongside nephrotic syndrome relapse two years after onset...After bendamustine-rituximab therapy showed partial effectiveness, tirabrutinib, a Bruton tyrosine kinase inhibitor, achieved complete remission of both renal and neurological manifestations with sustained response over three years. Immunofluorescence staining revealed increased nuclear factor (NF)-κB and STAT3 expression in infiltrating immune cells and elevated NF-κB in surrounding tubular epithelial cells, suggesting activation of these pathways downstream of the MYD88 mutation in kidney pathology. Our findings suggest a potential contribution of Bruton's tyrosine kinase signaling to both kidney and neurological pathology in Bing-Neel syndrome, with tirabrutinib achieving clinical improvement in both organ manifestations.
Journal
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MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • STAT3 (Signal Transducer And Activator Of Transcription 3)
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Rituxan (rituximab) • bendamustine • Velexbru (tirabrutinib)
4ms
New P3 trial
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Rituxan (rituximab) • temozolomide • Velexbru (tirabrutinib)
6ms
Phase I Study Evaluating Tolerability, Safety, Pharmacokinetics, and Efficacy of Combined ONO-4059 and R-MPV Therapy for PCNSL (clinicaltrials.gov)
P1, N=20, Active, not recruiting, Ono Pharmaceutical Co. Ltd | Recruiting --> Active, not recruiting
Enrollment closed
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Rituxan (rituximab) • vincristine • Matulane (procarbazine hydrochloride) • Velexbru (tirabrutinib)
7ms
Tirabrutinib-associated toxic epidermal necrolysis: a case report and review of the literature. (PubMed, Skin Health Dis)
Tirabrutinib's selective BTK inhibition may activate cytotoxic CD8+ T cells, contributing to Stevens-Johnson syndrome/TEN pathogenesis. Further studies are needed to clarify the mechanisms and develop better diagnostic approaches for BTK inhibitor-related drug eruptions.
Journal
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CD8 (cluster of differentiation 8)
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Velexbru (tirabrutinib)
7ms
Chronic expanding hematoma following Gamma Knife irradiation for primary central nervous system lymphoma: illustrative case. (PubMed, J Neurosurg Case Lessons)
In this patient, CEH could have resulted from VEGFR-1 expression due to GKRS. For a patient with slow lesion growth following GKRS for PCNSL, surgical removal should be considered, taking into account the possibility of CEH along with recurrence and radiation necrosis. https://thejns.org/doi/10.3171/CASE258.
Journal
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FLT1 (Fms-related tyrosine kinase 1)
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Rituxan (rituximab) • methotrexate • vincristine • Matulane (procarbazine hydrochloride) • Velexbru (tirabrutinib)
7ms
New P2 trial
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Velexbru (tirabrutinib)
8ms
RalB promotes lymph node metastasis in tongue squamous cell carcinoma. (PubMed, Genes Genomics)
RalB act as a prognostic gene in HNSCC, and promote lymph node metastasis in early stage of TSCC.
Journal
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RAS (Rat Sarcoma Virus) • RALB (RAS Like Proto-Oncogene B) • RRAGD (Ras related GTP binding)
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Velexbru (tirabrutinib)