^
    23h
    Genetic modulation of ABCB1: Sunvozertinib reverses ABCB1-mediated multidrug resistance in cancer cells. (PubMed, Cancer Genet)
    Furthermore, treatment with sunvozertinib did not change protein expression or subcellular localization of ABCB1. Altogether, these data demonstrate that sunvozertinib, when combined with other conventional chemotherapeutic agents, can overcome MDR and improve therapeutic effect.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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    EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
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    Zegfrovy (sunvozertinib)
    1d
    A Study to Investigate Sonrotoclax (BGB-11417) Plus Zanubrutinib (BGB-3111) Compared With Venetoclax Plus Acalabrutinib in Adults With Previously Untreated Chronic Lymphocytic Leukemia (clinicaltrials.gov)
    P3, N=500, Not yet recruiting, BeOne Medicines
    New P3 trial
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    Venclexta (venetoclax) • Brukinsa (zanubrutinib) • Calquence (acalabrutinib) • sonrotoclax (BGB-11417)
    1d
    KEYNOTE145: ACP-196 (Acalabrutinib) in Combination With Pembrolizumab, for Treatment of Hematologic Malignancies (clinicaltrials.gov)
    P1/2, N=161, Completed, Acerta Pharma BV | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Oct 2025
    Trial completion • Trial completion date
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    Keytruda (pembrolizumab) • Calquence (acalabrutinib)
    1d
    Is Bruton tyrosine kinase a potential target to treat mast cell neoplasms? Systemic mastocytosis associated with chronic lymphoid leukemia successfully treated with acalabrutinib monotherapy: a case report and review of the literature. (PubMed, Haematologica)
    Not available.
    Journal
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    BTK (Bruton Tyrosine Kinase)
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    Calquence (acalabrutinib)
    1d
    Exploratory Covalent Docking of Michael-Acceptor Natural Products at Reactive Cysteines in Cancer Tyrosine Kinases. (PubMed, Int J Mol Sci)
    Reference inhibitors (osimertinib-EGFR, ibrutinib-BTK, THZ1-CDK7, and THZ531-CDK12) reproduced the expected geometries and served as internal controls. Although no quantitative affinity was inferred, the consistent geometric feasibility supports their potential as structural templates for covalent-binding natural scaffolds. These results provide a qualitative, structure-based rationale for further chemoproteomic and enzymatic validation of NP-derived or hybrid compounds as potential leads in cancer therapy, expanding covalent chemical space beyond existing synthetic scaffolds.
    Journal
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    EGFR (Epidermal growth factor receptor) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CDK12 (Cyclin dependent kinase 12) • CDK7 (Cyclin Dependent Kinase 7)
    |
    Tagrisso (osimertinib) • Imbruvica (ibrutinib)
    2d
    Neoadjuvant Sunvozertinib in Stage II-IIIB Non-small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutation. (clinicaltrials.gov)
    P2, N=24, Active, not recruiting, Shanghai Pulmonary Hospital, Shanghai, China
    New P2 trial
    |
    Zegfrovy (sunvozertinib)
    3d
    Acalabrutinib (ACP-196) in Combination With ACP-319, for Treatment of B-Cell Malignancies (clinicaltrials.gov)
    P1/2, N=40, Completed, Acerta Pharma BV | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Oct 2025
    Trial completion • Trial completion date
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    Calquence (acalabrutinib) • ACP-319
    3d
    REL overexpression and sustained NF-κB signaling associated with 2p gain induce resistance to BTK inhibitors in Chronic Lymphocytic Leukemia. (PubMed, Leukemia)
    Moreover, upon ibrutinib treatment, REL DNA-binding activity decreased in 2pWT CLL cells but remained sustained in 2p+ CLL cells following BCR stimulation, suggesting that persistent NF-κB activation contributes to resistance...Altogether, our study identifies REL overexpression as a novel 2p+-driven mechanism of BTKi resistance in CLL, complementing the well described BTK and PLCG2 mutations. These findings support the clinical relevance of detecting 2p gain to guide treatment strategies and improve outcomes in CLL.
    Journal
    |
    PLCG2 (Phospholipase C Gamma 2) • REL (REL Proto-Oncogene)
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    Imbruvica (ibrutinib)
    3d
    Orelabrutinib Plus Lisaftoclax and Rituximab in Untreated Mantle Cell Lymphoma With High-Risk Disease (clinicaltrials.gov)
    P2, N=25, Recruiting, Ruijin Hospital
    New P2 trial
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    BCL2 (B-cell CLL/lymphoma 2)
    |
    Rituxan (rituximab) • Inokai (orelabrutinib) • lisaftoclax (APG-2575)
    3d
    A Study of Emavusertib + An Approved Bruton Tyrosine Kinase Inhibitor (BTKi) in Participants With Chronic Lymphocytic Leukemia (CLL) and Other B-cell Malignancies (clinicaltrials.gov)
    P2, N=108, Not yet recruiting, Curis, Inc.
    New P2 trial
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    Brukinsa (zanubrutinib) • emavusertib (CA-4948)
    3d
    BRUIN CLL-313: Randomized Phase III Trial of Pirtobrutinib Versus Bendamustine Plus Rituximab in Untreated Patients With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma. (PubMed, J Clin Oncol)
    Pirtobrutinib demonstrated superiority over BendaR in IRC-assessed PFS in treatment-naïve CLL/SLL. OS trends favored pirtobrutinib despite the study design allowing for crossover. Pirtobrutinib was well tolerated, consistent with its known safety profile, and more favorable than BendaR.
    P3 data • Journal • IO biomarker
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    IGH (Immunoglobulin Heavy Locus)
    |
    IGH mutation
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    Rituxan (rituximab) • Jaypirca (pirtobrutinib) • bendamustine
    4d
    Zanubrutinib Combined With Rituximab in the Treatment of Secondary HLH in B-cell Lymphoma (clinicaltrials.gov)
    P4, N=40, Recruiting, The First Affiliated Hospital of Soochow University
    New P4 trial
    |
    Rituxan (rituximab) • Jakafi (ruxolitinib) • Brukinsa (zanubrutinib)