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Casein kinase I epsilon inhibitor

7ms
Investigating Overlapping Immune-related Genetic Markers in Cholangiocarcinoma and Inflammatory Bowel Disease for Predictive Prognosis. (PubMed, J Immunother)
This study also predicted potential small molecule drugs that might be effective for the treatment of CHOL, such as Umbralisib and Tamoxifen. In conclusion, this study provides new biomarkers and potential targets for diagnosis, prognosis assessment, and treatment of CHOL and IBD.
Journal
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SPP1 (Secreted Phosphoprotein 1) • CCR7 (Chemokine (C-C motif) receptor 7) • OSMR (Oncostatin M Receptor) • PIK3R3 (Phosphoinositide-3-Kinase Regulatory Subunit 3) • S100P (S100 calcium binding protein P)
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tamoxifen • Ukoniq (umbralisib)
7ms
TLB-001 safety and tolerability study (ACTRN12624000813583)
P1, N=64, Completed, Tianli Biotech Pty Ltd | Recruiting --> Completed
Trial completion
8ms
A Double-blineded, Randomized, Multi-center Phase III Clinical Study of HZ-H08905 Versus Chidamide in Patients With Relapsed/Refractory PTCL (ChiCTR2500098784)
P3, N=140, Recruiting, Beijing Cancer Hospital/The First Affiliated Hospital of Zhejiang University School of Medicine; Hangzhou HealZen Therapeutics Co., Ltd
New P3 trial
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ALK (Anaplastic lymphoma kinase) • TNFRSF8 (TNF Receptor Superfamily Member 8)
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ALK positive • TNFRSF8 positive
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Epidaza (chidamide)
10ms
Treatment of Relapsed/Refractory CLL Patients With PI3Kδ Inhibitor and Anti-CD20 Antibody Rapidly Decreases Tumor Burden but Could Induce Resistance. (PubMed, Am J Hematol)
The clinical trial utilized 1)a therapeutic anti-CD20 monoclonal antibody (mAb), ublituximab, which destroys CLL cells by an antibody-dependent cellular phagocytosis (ADCP) mechanism; 2)a B cell receptor (BCR) signaling inhibitor, umbralisib, which blocks PI3Kẟ; 3)and an anti-apoptosis inhibitor, venetoclax, which blocks cell survival promoted by BCL-2 that stops mitochondria from initiating apoptosis. Standard high dose (375 mg/m2) anti-CD20 antibody treatment significantly decreased CLL surface CD20 levels, potentially limiting treatment efficacy. Anti-CD20 antibody plus B cell receptor signaling inhibition reduced CLL cell counts and lymph node tumors, enabling BCL-2 inhibitor treatment to avoid tumor lysis syndrome.
Journal
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PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
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Venclexta (venetoclax) • Ukoniq (umbralisib) • Briumvi (ublituximab-xiiy)
1year
Acalabrutinib, Umbralisib and Ublituximab Regimen (AU2) Demonstrates High Response Rate and Undetectable Molecular Minimal Residual Disease (MRD) in Patients (pts) with De Novo Mantle Cell Lymphoma (MCL) (ASH 2024)
Two pts were switched to zanubrutinib due to PD on U2, both achieved response. AU2 is a highly effective regimen in pts with previously untreated MCL, including those with high-risk genetics (100% CR rate), and achieves a high molecular uMRD rate. Pts who develop progressive disease can be effectively salvaged with subsequent therapies.
Clinical • IO biomarker • Minimal residual disease
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TP53 (Tumor protein P53)
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TP53 mutation
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clonoSEQ
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Brukinsa (zanubrutinib) • Calquence (acalabrutinib) • Ukoniq (umbralisib) • Briumvi (ublituximab-xiiy)
1year
Acalabrutinib, Umbralisib, and Ublituximab (AU2) In Relapsed and Untreated CLL (clinicaltrials.gov)
P2, N=60, Active, not recruiting, Jennifer R. Brown, MD, PhD | Trial primary completion date: Dec 2023 --> Dec 2026
Trial primary completion date
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Calquence (acalabrutinib) • Ukoniq (umbralisib) • Briumvi (ublituximab-xiiy)
1year
Acalabrutinib, Umbralisib, and Ublituximab (AU2) In Relapsed and Untreated CLL (clinicaltrials.gov)
P2, N=60, Active, not recruiting, Jennifer R. Brown, MD, PhD | Trial primary completion date: Jan 2025 --> Dec 2023
Trial primary completion date
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Calquence (acalabrutinib) • Ukoniq (umbralisib) • Briumvi (ublituximab-xiiy)
1year
TLB-001 safety and tolerability study (ACTRN12624000813583)
P1, N=64, Recruiting, Tianli Biotech Pty Ltd | Not yet recruiting --> Recruiting
Enrollment open • Trial initiation date
over1year
Enrollment closed
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CD4 (CD4 Molecule)
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lenalidomide • doxorubicin hydrochloride • Gazyva (obinutuzumab) • cyclophosphamide • vincristine • Ukoniq (umbralisib) • Belrapzo (bendamustine RTD)
over1year
Evaluate the Efficacy and Safety of TGR-1202 in Participants With Chronic Lymphocytic Leukemia Who Are Intolerant to Prior Therapy (clinicaltrials.gov)
P2, N=51, Terminated, TG Therapeutics, Inc. | Completed --> Terminated; (Strategic/Business Decision)
Trial termination
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Ukoniq (umbralisib)
over1year
TGR-1202 + Ruxolitinib PMF PPV-MF PET-MF MDS/MPN Polycythemia Vera Resistant to Hydroxyurea (clinicaltrials.gov)
P1, N=60, Completed, Vanderbilt-Ingram Cancer Center | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> May 2024
Trial completion • Trial completion date
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Jakafi (ruxolitinib) • Ukoniq (umbralisib) • hydroxyurea
over1year
A Phase I/Ib Safety and Efficacy Study of the PI3K-delta Inhibitor TGR-1202 and Ibrutinib in Patients With CLL or MCL (clinicaltrials.gov)
P1, N=45, Completed, Dana-Farber Cancer Institute | Active, not recruiting --> Completed | Trial completion date: Mar 2024 --> Aug 2023
Trial completion • Trial completion date • Combination therapy
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Imbruvica (ibrutinib) • Ukoniq (umbralisib)