^
    14h
    ALLIANCE A041202: Rituximab and Bendamustine Hydrochloride, Rituximab and Ibrutinib, or Ibrutinib Alone in Treating Older Patients With Previously Untreated Chronic Lymphocytic Leukemia (clinicaltrials.gov)
    P3, N=547, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jan 2025 --> Jan 2026
    Trial completion date
    |
    CD20 (Membrane Spanning 4-Domains A1) • CD4 (CD4 Molecule) • CD5 (CD5 Molecule) • FCER2 (Fc Fragment Of IgE Receptor II)
    |
    Chr t(11;14)
    |
    Imbruvica (ibrutinib) • Rituxan (rituximab) • bendamustine • Truxima (rituximab-abbs) • Belrapzo (bendamustine RTD) • Mabtas (rituximab biosimilar)
    3d
    Study of Remibrutinib (LOU064) Efficacy and Safety and Exploration of Its Mechanism of Action in Participants With Chronic Urticaria (clinicaltrials.gov)
    P2, N=44, Not yet recruiting, Novartis Pharmaceuticals
    New P2 trial
    |
    remibrutinib (LOU064)
    3d
    A Phase 2 Trial of Mosunetuzumab and Zanubrutinib for Patients With Relapsed/Refractory Marginal Zone Lymphoma (clinicaltrials.gov)
    P2, N=36, Recruiting, M.D. Anderson Cancer Center | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Brukinsa (zanubrutinib) • Lunsumio (mosunetuzumab-axgb)
    4d
    RECHARGE 2: Study to Assess Efficacy Safety and Tolerability of Remibrutinib in Adult Patients With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P3, N=555, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    remibrutinib (LOU064)
    4d
    RECLAIM: A Study to Evaluate Efficacy of Remibrutinib Compared to Dupilumab at Early Timepoints in Adults With Chronic Spontaneous Urticaria Inadequately Controlled by Second Generation H1-antihistamines (clinicaltrials.gov)
    P3, N=400, Not yet recruiting, Novartis Pharmaceuticals
    New P3 trial
    |
    remibrutinib (LOU064) • Dupixent (dupilumab)
    6d
    A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of HS-10561 Capsule in Healthy Chinese Adults and Patients With Chronic Spontaneous Urticaria. (clinicaltrials.gov)
    P1/2, N=150, Not yet recruiting, Jiangsu Hansoh Pharmaceutical Co., Ltd.
    New P1/2 trial
    |
    rocbrutinib (LP-168)
    6d
    Nemtabrutinib and Pembrolizumab for the Treatment of Richter Transformation, Diffuse Large B-cell Lymphoma Subtype (clinicaltrials.gov)
    P2, N=32, Not yet recruiting, Roswell Park Cancer Institute
    New P2 trial • Tumor mutational burden
    |
    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • nemtabrutinib (MK-1026)
    6d
    An Extension Study of Long-term Efficacy, Safety and Tolerability of Remibrutinib in Chronic Spontaneous Urticaria Patients Who Completed Preceding Studies With Remibrutinib (clinicaltrials.gov)
    P3, N=694, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Feb 2027 --> Aug 2027
    Trial completion date
    |
    remibrutinib (LOU064)
    7d
    WU-KONG20: Perioperative Treatment of Sunvozertinib in Stage II-IIIB NSCLC (clinicaltrials.gov)
    P2, N=27, Recruiting, Tang-Du Hospital
    New P2 trial
    |
    sunvozertinib (DZD9008)
    7d
    A Study of CG-806 in Patients With Relapsed or Refractory AML or Higher-Risk MDS (clinicaltrials.gov)
    P1, N=45, Terminated, Aptose Biosciences Inc. | N=80 --> 45 | Trial completion date: May 2025 --> Apr 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2024 --> Apr 2024; Change in corporate strategy
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    luxeptinib (CG-806)
    7d
    RELIEVE: A Study to Investigate the Efficacy, Safety and Tolerability of Remibrutinib Versus Placebo in Adult Patients With Generalized Myasthenia Gravis (clinicaltrials.gov)
    P3, N=180, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    remibrutinib (LOU064)
    7d
    A Study of CG-806 in Patients With Relapsed or Refractory CLL/SLL or Non-Hodgkin's Lymphomas (clinicaltrials.gov)
    P1, N=36, Terminated, Aptose Biosciences Inc. | N=160 --> 36 | Trial completion date: May 2025 --> May 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2024 --> May 2024; Change in corporate strategy
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    luxeptinib (CG-806)
    8d
    Zanubrutinib in Combination With Sonrotoclax for the Treatment of Underrepresented Ethnic and Racial Minorities With Relapsed or Refractory B-cell Non-Hodgkin Lymphoma (clinicaltrials.gov)
    P1, N=37, Not yet recruiting, City of Hope Medical Center
    New P1 trial
    |
    Brukinsa (zanubrutinib) • sonrotoclax (BGB-11417)
    9d
    A Study on Limiting Treatment Time With Acalabrutinib Combined With Obinutuzumab in People With CLL or SLL (clinicaltrials.gov)
    P2, N=55, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Feb 2025 --> Feb 2026 | Trial primary completion date: Feb 2025 --> Feb 2026
    Trial completion date • Trial primary completion date • Minimal residual disease
    |
    Gazyva (obinutuzumab) • Calquence (acalabrutinib)
    9d
    Clinical Trial of TQB3702 Tablets in Subjects With Systemic Lupus Erythematosus (SLE) (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    New P2 trial
    9d
    Pembrolizumab, Ibrutinib and Rituximab in PCNSL (clinicaltrials.gov)
    P1/2, N=37, Recruiting, Dana-Farber Cancer Institute | Trial completion date: Mar 2025 --> Jan 2026 | Trial primary completion date: Feb 2025 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    Keytruda (pembrolizumab) • Imbruvica (ibrutinib) • Rituxan (rituximab) • Truxima (rituximab-abbs)
    9d
    Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties. (PubMed, Eur J Med Chem)
    Based on noncovalent inhibitor ARQ-531, we previously developed two potent BTK PROTACs 6e and SC-3e, which exhibited poor pharmacokinetic property...Furthermore, compound 27 displayed excellent cell antiproliferative activities, metabolic stability in mouse liver microsomes and improved bioavailability in mice. Overall, 27 is a highly effective and selective BTK degrader that is suitable for in vivo efficacy investigations.
    PK/PD data • Journal
    |
    BTK (Bruton Tyrosine Kinase) • CRBN (Cereblon)
    |
    BTK C481S
    |
    nemtabrutinib (MK-1026)
    10d
    BTK inhibitors enhance NKG2D ligand expression by regulating IL-10/STAT3 pathway in activated non-GCB diffuse large B-cell lymphoma cells. (PubMed, Anticancer Drugs)
    In contrast, treatment with ibrutinib produced effects opposite to those induced by IgM antibodies. Similar outcomes were observed when the BTK inhibitors ACP-196 and BGB-3111 were administered. Our findings suggest that the IL-10/STAT3 pathway plays a key role in the upregulation of NKG2D ligands induced by BTK inhibitors in U2932 and OCI-LY3 cells.
    Journal
    |
    IL10 (Interleukin 10) • NKG2D (killer cell lectin like receptor K1) • ULBP2 (UL16 Binding Protein 2)
    |
    Imbruvica (ibrutinib) • Brukinsa (zanubrutinib) • Calquence (acalabrutinib)
    10d
    Design and application of a fluorescent probe for imaging of endogenous Bruton's tyrosine kinase with preserved enzymatic activity. (PubMed, RSC Chem Biol)
    Evobrutinib, a second-generation BTK inhibitor with high selectivity, was chosen as the scaffold...The dynamic signalling pathway of BTK in its native environment was investigated by confocal microscopy with Evo-2. This methodology is a valuable asset in the chemical biology toolbox for studying protein dynamics and interactions in real time without interfering with the protein activity.
    Journal
    |
    BTK (Bruton Tyrosine Kinase)
    11d
    A Study to Investigate the Efficacy and Safety of Sonrotoclax Plus Zanubrutinib Compared With Placebo Plus Zanubrutinib in Adults With Relapsed/Refractory Mantle Cell Lymphoma (clinicaltrials.gov)
    P3, N=300, Recruiting, BeiGene | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Brukinsa (zanubrutinib) • sonrotoclax (BGB-11417)
    11d
    BCL-2 dependence is a favorable predictive marker of response to therapy for chronic lymphocytic leukemia. (PubMed, Mol Cancer)
    We comprehensively defined BCL-2 dependence as a potential functional and predictive biomarker of treatment response in CLL, underscoring the importance of characterizing apoptotic signaling in CLL to stratify patients beyond genetic markers and identifying novel combinations to exploit BCL-2 dependence therapeutically. Our approach has the potential to help optimize targeted therapy combinations for CLL patients.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    Imbruvica (ibrutinib) • Rituxan (rituximab) • cyclophosphamide • fludarabine IV
    13d
    Efficacy, Safety and Pharmacokinetics of Rilzabrutinib in Patients With Warm Autoimmune Hemolytic Anemia (wAIHA) (clinicaltrials.gov)
    P2, N=22, Active, not recruiting, Sanofi | Trial completion date: May 2025 --> Dec 2029
    Trial completion date
    13d
    Ipilimumab, Ibrutinib, and Nivolumab for the Treatment of Chronic Lymphocytic Leukemia and Richter Transformation (clinicaltrials.gov)
    P1, N=0, Withdrawn, M.D. Anderson Cancer Center | N=50 --> 0 | Trial completion date: Dec 2025 --> Feb 2025 | Active, not recruiting --> Withdrawn | Trial primary completion date: Dec 2025 --> Feb 2025
    Enrollment change • Trial completion date • Trial withdrawal • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • Imbruvica (ibrutinib)
    14d
    BOSon: Zanubrutinib, Obinutuzumab, and Sonrotoclax in Previously Untreated Patients with CLL or SLL (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Massachusetts General Hospital
    New P2 trial
    |
    Gazyva (obinutuzumab) • Brukinsa (zanubrutinib) • sonrotoclax (BGB-11417)
    14d
    Plasma Membrane Targeted Photodynamic Nanoagonist to Potentiate Immune Checkpoint Blockade Therapy by Initiating Tumor Cell Pyroptosis and Depleting Infiltrating B Cells. (PubMed, Adv Mater)
    PMTPN is composed of a rationally designed chimeric peptide sequence loaded with Bruton's tyrosine kinase inhibitor (Ibrutinib)...Beneficially, the synergistic immune modulating characteristics of PMTPN potentiate ICB therapy to simultaneously eliminate primary and distant tumors. This study offers a promising strategy to elevate the immunotherapeutic response rate in consideration of the complex immunosuppressive factors.
    Journal • Checkpoint inhibition
    |
    IL10 (Interleukin 10)
    |
    Imbruvica (ibrutinib)
    15d
    Rituxan/Bendamustine/PCI-32765 in Relapsed DLBCL, MCL, or Indolent Non-Hodgkin's Lymphoma (clinicaltrials.gov)
    P1, N=48, Active, not recruiting, Kami Maddocks, MD | Trial completion date: Dec 2024 --> May 2025 | Trial primary completion date: Mar 2014 --> May 2025
    Trial completion date • Trial primary completion date
    |
    Imbruvica (ibrutinib) • Rituxan (rituximab) • bendamustine
    15d
    Acalabrutinib With or Without Obinutuzumab in Treating Patients With Early-Stage Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma (clinicaltrials.gov)
    P2, N=120, Recruiting, Mayo Clinic | Trial completion date: Mar 2031 --> Oct 2031 | Trial primary completion date: Mar 2030 --> Oct 2030
    Trial completion date • Trial primary completion date
    |
    CD20 (Membrane Spanning 4-Domains A1) • CCND1 (Cyclin D1) • CD5 (CD5 Molecule) • FCER2 (Fc Fragment Of IgE Receptor II)
    |
    Chr t(11;14)
    |
    Gazyva (obinutuzumab) • Calquence (acalabrutinib)
    15d
    Zanubrutinib in Patients With DLBCL and MYD88 or NOTCH1 Mutation or CD5+ (clinicaltrials.gov)
    P2, N=21, Not yet recruiting, Virginia Commonwealth University
    New P2 trial
    |
    BCL2 (B-cell CLL/lymphoma 2) • NOTCH1 (Notch 1) • MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • CD79B (CD79b Molecule) • CD5 (CD5 Molecule)
    |
    doxorubicin hydrochloride • cyclophosphamide • Brukinsa (zanubrutinib)
    15d
    OSU-16077: Ibrutinib and Nivolumab in Treating Patients with Relapsed or Refractory Classical Hodgkin Lymphoma (clinicaltrials.gov)
    P2, N=18, Active, not recruiting, Ohio State University Comprehensive Cancer Center | Trial completion date: Dec 2024 --> May 2025 | Trial primary completion date: Dec 2024 --> May 2025
    Trial completion date • Trial primary completion date
    |
    Opdivo (nivolumab) • Imbruvica (ibrutinib)
    15d
    Efficacy and Safety of Remibrutinib After Switching From Ocrelizumab in Participants Living With Relapsing Multiple Sclerosis. (clinicaltrials.gov)
    P3, N=360, Not yet recruiting, Novartis Pharmaceuticals
    New P3 trial • Head-to-Head
    |
    remibrutinib (LOU064) • Ocrevus (ocrelizumab)
    15d
    Acalabrutinib Plus Rituximab for the Treatment of Elderly or Low- to Intermediate-Risk Younger Untreated Mantle Cell Lymphoma (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, Sun Yat-sen University
    New P2 trial
    |
    Rituxan (rituximab) • Calquence (acalabrutinib)
    15d
    Assessing an Oral Bruton Tyrosine Kinase Inhibitor, DZD9008 in Patients Who Have Non-Hodgkin B-cell Lymphoma (WU-KONG3) (clinicaltrials.gov)
    P1/2, N=0, Withdrawn, Dizal Pharmaceuticals | N=120 --> 0 | Suspended --> Withdrawn
    Enrollment change • Trial withdrawal
    |
    sunvozertinib (DZD9008)
    15d
    Design, synthesis and anti-tumor activity of BTK inhibitor Orelabrutinib derivatives. (PubMed, Bioorg Chem)
    Using scaffold hopping strategies, 28 novel derivatives belonging to the tricyclic and pyridine amide series were designed and synthesized from the lead compound Orelabrutinib. The outcomes revealed that 11a and 11k were able to effectively restrain the growth and migration of the tumor cell TMD8 upon comparing their in vitro activities, meriting further examination.
    Journal
    |
    BTK (Bruton Tyrosine Kinase)
    |
    Inokai (orelabrutinib)
    17d
    Safety and Efficacy of Zanubrutinib in the Treatment of Antiphospholipid Syndrome With Secondary Thrombocytopenia (clinicaltrials.gov)
    P2, N=10, Recruiting, Institute of Hematology & Blood Diseases Hospital, China | Trial completion date: Jun 2024 --> Jun 2025
    Trial completion date
    |
    Brukinsa (zanubrutinib)
    17d
    Acalabrutinib Monotherapy vs Investigator's Choice of Treatment in Patients With CL Leukaemia and Heart Failure (clinicaltrials.gov)
    P4, N=60, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Venclexta (venetoclax) • Rituxan (rituximab) • Gazyva (obinutuzumab) • Brukinsa (zanubrutinib) • Calquence (acalabrutinib)
    18d
    Acalabrutinib With or Without Obinutuzumab in Treating Patients With Early-Stage Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma (clinicaltrials.gov)
    P2, N=120, Recruiting, Mayo Clinic | Trial completion date: Mar 2026 --> Mar 2031 | Trial primary completion date: Mar 2025 --> Mar 2030
    Trial completion date • Trial primary completion date
    |
    CD20 (Membrane Spanning 4-Domains A1) • CCND1 (Cyclin D1) • CD5 (CD5 Molecule) • FCER2 (Fc Fragment Of IgE Receptor II)
    |
    Chr t(11;14)
    |
    Gazyva (obinutuzumab) • Calquence (acalabrutinib)
    18d
    A Prospective, One-arm and Open Clinical Study of Zanubrutinib in the Treatment of Immune Thrombocytopenia (clinicaltrials.gov)
    P2, N=30, Recruiting, Institute of Hematology & Blood Diseases Hospital, China | Trial completion date: Jun 2024 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    Brukinsa (zanubrutinib)
    20d
    Sonrotoclax, Rituximab, and Zanubrutinib in Treating Participants With Chronic Lymphocytic Leukemia, Small Lymphocytic Lymphoma, and Mantle Cell Lymphoma (clinicaltrials.gov)
    P2, N=20, Not yet recruiting, Fred Hutchinson Cancer Center
    New P2 trial
    |
    Rituxan (rituximab) • Brukinsa (zanubrutinib) • Truxima (rituximab-abbs) • sonrotoclax (BGB-11417) • Mabtas (rituximab biosimilar)
    20d
    A Study of DZD8586 in Relapsed or Refractory B-Cell Non-Hodgkin Lymphoma (TAI-SHAN1) (clinicaltrials.gov)
    P1/2, N=17, Completed, Dizal Pharmaceuticals | Recruiting --> Completed | N=386 --> 17 | Trial completion date: Oct 2027 --> Feb 2024 | Trial primary completion date: Apr 2027 --> Feb 2024
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    DZD8586
    21d
    BOSS: A Study to Investigate the Sequencing Strategy of Pirtobrutinib After Disease Progression on First-line Acalabrutinib Treatment for Adult Participants With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma (clinicaltrials.gov)
    P2, N=60, Not yet recruiting, AstraZeneca
    New P2 trial
    |
    Calquence (acalabrutinib) • Jaypirca (pirtobrutinib)
    21d
    RECHARGE 2: Study to Assess Efficacy Safety and Tolerability of Remibrutinib in Adult Patients With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov)
    P3, N=555, Not yet recruiting, Novartis Pharmaceuticals
    New P3 trial
    |
    remibrutinib (LOU064)
    21d
    Fixed-Duration Acalabrutinib Combinations in Untreated Chronic Lymphocytic Leukemia. (PubMed, N Engl J Med)
    Acalabrutinib-venetoclax with or without obinutuzumab significantly prolonged progression-free survival as compared with chemoimmunotherapy in fit patients with previously untreated CLL. (Funded by AstraZeneca; AMPLIFY ClinicalTrials.gov number, NCT03836261.).
    Clinical • Journal • IO biomarker
    |
    TP53 (Tumor protein P53) • IGH (Immunoglobulin Heavy Locus)
    |
    TP53 mutation
    |
    Venclexta (venetoclax) • Rituxan (rituximab) • Gazyva (obinutuzumab) • cyclophosphamide • Calquence (acalabrutinib) • bendamustine • fludarabine IV