Inokai (orelabrutinib) / InnoCare, Zenas BioPharma - LARVOL DELTA

Orelabrutinib plus Rituximab Maintenance after Short-Course Chemoimmunotherapy in Intermediate/High-Risk Marginal Zone Lymphoma (ESMO 2026) - No abstract available

Clinical • Hematological Malignancies • Lymphoma • Marginal Zone Lymphoma • Oncology

Sustained Benefit of Orelabrutinib in Relapsed/Refractory Chronic Lymphocytic Leukemia: Up to 5 Years of Follow-Up from a Phase 2 Study (ESMO 2026) - No abstract available

P2 data • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Oncology

Orelabrutinib, Lenalidomide, and Rituximab as Frontline Therapy for Mantle Cell Lymphoma: Results of the Phase II POLARIS Study (ESMO 2026) - No abstract available

P2 data • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Oncology

A Phase II Trial of Orelabrutinib Combined with New CD20 Monoclonal Antibody in Previously Untreated Marginal Zone Lymphoma: A Multicenter, Single-Arm Study (ZOOM Trial) Results Update (ESMO 2026) - No abstract available

Clinical • P2 data • Hematological Malignancies • Lymphoma • Marginal Zone Lymphoma • Oncology

BTK Inhibitors Combined With High-Dose Methotrexate–Based Induction in Newly Diagnosed Primary CNS Lymphoma: A Systematic Review and Meta-Analysis (SOHO 2026) - "We performed a systematic review and meta-analysis to estimate the efficacy and safety of covalent Bruton tyrosine kinase (BTK) inhibitors (ibrutinib, zanubrutinib, and orelabrutinib) added to HD-MTX–based induction in newly diagnosed PCNSL. BTK inhibitor–augmented HD-MTX induction achieved an ORRof 89% and CR rate of 67%, with a 2-year PFS of 67% and OS of 84%, thus outperforming HD-MTX alone. Toxicity was manageable, with minimal atrial fibrillation and no invasive fungal infections. Further studies are needed to define its role in combination strategies."

Retrospective data • Review • B Cell Lymphoma • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Primary Central Nervous System Lymphoma

BTK and BCL2 targeting with orelabrutinib (ICP-022) and mesutoclax (ICP-248): single-agent and combination activity in marginal zone lymphoma, including drug-resistant derivatives (EORTC-NCI-AACR 2026) - "Abstract will be available as of 4 November (with consent of the author)"

Hematological Malignancies • Lymphoma • Marginal Zone Lymphoma • Oncology • BCL2

Rituximab, high-dose methotrexate plus orelabrutinib as induction therapy in newly diagnosed primary central nervous system lymphoma. (PubMed, Leukemia) - No abstract available

Journal • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Primary Central Nervous System Lymphoma

Orelabrutinib versus chemoimmunotherapy in treatment-naïve chronic lymphocytic leukemia/small lymphocytic lymphoma: a randomized, phase 3 trial. (PubMed, Signal Transduct Target Ther) - P3 | "From February 20, 2021, to July 8, 2024, 192 eligible patients were randomly assigned (1:1) to receive either orelabrutinib (91 patients) or chlorambucil plus rituximab (101 patients), comprising the intention-to-treat population. Orelabrutinib maintained or improved patient-reported outcomes compared with chemoimmunotherapy. In summary, orelabrutinib significantly improved PFS and response versus chemoimmunotherapy in patients with treatment-naïve CLL/SLL, with a manageable safety profile, supporting it as an effective alternative first-line option."

Clinical • Journal • P3 data • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma

Titanium-catalyzed Cross-coupling of Aryl Boronate Derivatives and Aryl Halides en Route to Biaryl Backbones. (PubMed, Org Lett) - "Its practical utility is highlighted by a gram-scale reaction and late-stage modifications, including the synthesis of an Orelabrutinib core intermediate. Preliminary mechanistic experiments, including radical-trapping, isotope-labeling, electrochemical, Hammett, and crossover studies, reveal reactivity features distinct from those commonly observed in conventional Suzuki-Miyaura cross-coupling. These observations provide experimental constraints for future mechanistic investigations of this titanium-catalyzed transformation."

Journal

Efficacy and Safety of Bruton's Tyrosine Kinase Inhibitors in Primary Immune Thrombocytopenia: A Systematic Review and Meta-Analysis (SOHO 2026) - "Objective: Assess pooled efficacy and safety of BTK inhibitors rilzabrutinib, zanubrutinib, and orelabrutinib in primary ITP. BTK inhibitors demonstrate appreciable platelet responses and a manageable safety profile across drug classes. Significant between-study heterogeneity warrants cautious interpretation. The August 2025 FDA approval of rilzabrutinib for ITP validates this class; however, comparative data and long-term durability evidence remain clinical priorities."

Retrospective data • Review • Oncology

Orelabrutinib Combined With Pola-R-CHP as First-Line Treatment for Patients With Intermediate- to High-Risk DLBCL (clinicaltrials.gov) - P=N/A | N=30 | Recruiting | Sponsor: The First Affiliated Hospital of Xiamen University

New trial • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • BCL2

ORMD2021: A Dose-escalating Pilot Study of Orelabrutinib for Newly-diagnosed PCNSL (clinicaltrials.gov) - P1 | N=13 | Completed | Sponsor: Huashan Hospital | Active, not recruiting ➔ Completed

Trial completion • B Cell Lymphoma • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Primary Central Nervous System Lymphoma

Orelabrutinib Combined With Teniposide, Rituximab and Methotrexate for Newly Diagnosed PCNSL (clinicaltrials.gov) - P2/3 | N=215 | Recruiting | Sponsor: Huashan Hospital | Not yet recruiting ➔ Recruiting

Enrollment open • B Cell Lymphoma • CNS Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Primary Central Nervous System Lymphoma

A Phase 3 Study to Compare the Efficacy of ICP-248 in Combination With Orelabrutinib Versus Pirtobrutinib in Participants With Relapsed or Refractory Mantle Cell Lymphoma (r/r MCL). (clinicaltrials.gov) - P3 | N=280 | Not yet recruiting | Sponsor: Beijing InnoCare Pharma Tech Co., Ltd.

New P3 trial • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Oncology

Orelabrutinib, fludarabine, cyclophosphamide, and obinutuzumab (OFCG) for first-line treatment of chronic lymphocytic leukemia: a multicenter phase II trial (cwCLL-001 trial). (PubMed, J Natl Cancer Cent) - P2 | "The study meet the primary endpoint, showing the potential efficacy and acceptable safety profile of the OFCG regimen as a first-line treatment for CLL. Trial registration: NCT05322733."

Journal • P2 data • Chronic Lymphocytic Leukemia • Hematological Disorders • Hematological Malignancies • Infectious Disease • Leukemia • Lymphoma • Neutropenia • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma • Thrombocytopenia • IGH • TP53

Orelabrutinib in combination with pomalidomide for the successful treatment of primary vitreoretinal lymphoma: a case report. (PubMed, Front Med (Lausanne)) - "Precise diagnosis and individualized treatment regimens are required for the therapy of PVRL. Besides, the orelabrutinib-pomalidomide combination represents a promising, well-tolerated targeted and chemo free therapy strategy for PVRL."

Journal • Cataract • CNS Lymphoma • Hematological Disorders • Hematological Malignancies • Infectious Disease • Keratitis • Lymphoma • Ocular Inflammation • Oncology • Ophthalmology • Primary Vitreoretinal Lymphoma • Respiratory Diseases • Uveitis • IL10

Four abstracts accepted for MSToronto 2026 including 24-week data and pharmacokinetic analysis from the orelabrutinib Phase 2 relapsing remitting multiple sclerosis trial along with study designs for the Phase 3 Monarch and PriMroSe trials (The Manila Times)

Clinical protocol • P2 data • Trial status • Immunology • Multiple Sclerosis

Approval of Orelabrutinib for the treatment of relapsed or refractory mantle cell lymphoma in Australia (InnoCare Pharma Press Release)

Approval • Mantle Cell Lymphoma

InnoCare Pharma…announced today that orelabrutinib, in combination with mesutoclax (ICP-248), has been granted Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) of the…NMPA for the treatment of patients with marginal zone lymphoma (MZL) who have received at least one prior therapy (PRNewswire) - "Data presented at the 2026 American Society of Clinical Oncology (ASCO) Annual Meeting demonstrated that orelabrutinib in combination with mesutoclax achieved excellent efficacy and safety in patients with MZL who had received at least one prior therapy, with an overall response rate (ORR) of 100%."

Breakthrough therapy • Non-US regulatory • Marginal Zone Lymphoma

Pretreatment With BTK Inhibitors Improved the Sensitivity of DLBCL Cells to CAR-T Cells in a Coculture System by Downregulating the Polarisation of M2 Macrophages. (PubMed, J Cell Mol Med) - "The cytotoxicity of CD19 CAR-T cells on HBL-1/U2932 cells pretreated with ibrutinib/orelabrutinib was higher than that of HBL-1/U2932 cells unpretreated with ibrutinib/orelabrutinib. Pretreatment with BTKi could down-regulate the polarisation of M2 macrophages and reverse the resistance of DLBCL cells which were cocultured with alternative activated M2 macrophages to CAR-T cells. This effect might be achieved by downregulating the Notch-RBP-J pathway."

IO biomarker • Journal • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • IL10 • MRC1 • NOTCH1

Orelabrutinib Combined With Obinutuzumab and Short-Course Venetoclax in Patients With Treatment-Nave Mantle Cell Lymphoma (MCL) (clinicaltrials.gov) - P2 | N=39 | Recruiting | Sponsor: The First Affiliated Hospital with Nanjing Medical University

New P2 trial • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Oncology • BCL2

A Multicenter, Prospective, Open-Label, Randomized Controlled Clinical Study of Orelabrutinib Combined With Obinutuzumab and Lenalidomide Versus Obinutuzumab Plus Chemotherapy for Treatment-Naive Follicular Lymphoma (clinicaltrials.gov) - P3 | N=652 | Not yet recruiting | Sponsor: Ruijin Hospital

New P3 trial • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Oncology

A Prospective Study of Response-adapted Low-dose Radiotherapy Combined With Orelabrutinib for Localized Mucosa-associated Lymphoid Tissue Extranodal Marginal Zone Lymphoma (clinicaltrials.gov) - P2 | N=140 | Not yet recruiting | Sponsor: Ruijin Hospital

New P2 trial • B Cell Lymphoma • Extranodal Marginal Zone Lymphoma • Hematological Malignancies • Lymphoma • Marginal Zone Lymphoma • Oncology

A UHPLC-MS/MS method for the simultaneous quantification of BTK inhibitors and their active metabolite in human plasma and cerebrospinal fluid. (PubMed, Bioanalysis) - "Bruton's tyrosine kinase inhibitors (BTKis, ibrutinib, zanubrutinib, orelabrutinib) are key targeted therapies for B-cell lymphomas, but interindividual variability and adverse reactions limit their use. The method was applied to 34 clinical samples (25 plasma, 9 CSF) from 20 patients. This method detects four BTK-related analytes in plasma/CSF with a 3-min run time, evaluation of hemolytic/lipemic matrices, and clinical validation, increasing throughput, reducing costs, and broadening applicability, providing preliminary feasibility data for clinical TDM."

Journal • B Cell Lymphoma • CNS Lymphoma • Hematological Malignancies • Hepatology • Liver Failure • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Immune thrombocytopenia: Evolving mechanistic understanding and clinical development of new therapies. (PubMed, Tzu Chi Med J) - "Although corticosteroids, intravenous immunoglobulin, anti-D immunoglobulin, rituximab, splenectomy, and thrombopoietin receptor agonists have constituted the therapeutic foundation for decades, these approaches remain limited by transient responses, toxicity, and insufficient disease modification...Bruton tyrosine kinase (BTK) inhibitors (rilzabrutinib and orelabrutinib) modulate B-cell activation and macrophage effector pathways; spleen tyrosine kinase inhibitors (fostamatinib) block Fcγ receptor-mediated phagocytosis, neonatal Fc receptor inhibitors (efgartigimod and rozanolixizumab) accelerate IgG catabolism and rapidly reduce pathogenic autoantibody burden; and complement inhibition (sutimlimab) provides a rational strategy for patients in whom classical pathway activation contributes to refractory disease. Collectively, these agents represent the most significant expansion of the ITP treatment landscape in decades, offering steroid-sparing options and enabling more..."

Journal • Review • Hematological Disorders • Immune Thrombocytopenic Purpura • Immunology • Thrombocytopenia • Thrombocytopenic Purpura