# Zanubrutinib

Source: https://onco.cc/drugs/zanubrutinib/  
OnCo record `zanubrutinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Zanubrutinib is the only BTK blocker to beat ibrutinib on both efficacy and safety in a head-to-head trial. It is now the most prescribed BTK inhibitor in CLL.

## Summary

ALPINE (relapsed CLL): PFS superior to ibrutinib (HR 0.65) with less atrial fibrillation; SEQUOIA (frontline): PFS superior to bendamustine-rituximab, 5-year PFS 72% in del(17p); SEQUOIA arm D (zanubrutinib + venetoclax) uMRD ~60%. Approved in CLL January 2023. Also MCL, Waldenström, MZL, follicular lymphoma. BeOne is testing zanubrutinib + sonrotoclax (CELESTIAL-TNCLL) and the BTK degrader BGB-16673 as successors.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-07
- Brand: Brukinsa
- Modality: Small-molecule covalent BTK inhibitor (second generation)
- Mechanism: Covalent BTK inhibitor with sustained near-complete BTK occupancy in lymph nodes and fewer off-target kinases than ibrutinib.
- Approvals: US 2019: Relapsed MCL (accelerated); US 2023: CLL/SLL, all lines (SEQUOIA, ALPINE)
- Dosing: Oral; 160 mg twice daily or 320 mg once daily, continuously
- Toxicity (grade 3+): Neutropenia 16%

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Zanubrutinib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Zanubrutinib

## Connected records

- cancers: [Chronic lymphocytic leukaemia](https://onco.cc/cancers/cll/), [Chronic lymphocytic leukaemia, first treatment](https://onco.cc/cancers/cll-treatment-naive/), [Diffuse large B-cell lymphoma](https://onco.cc/cancers/dlbcl/), [Extranodal marginal zone lymphoma of mucosa-associated lymphoid tissue (MALT lymphoma)](https://onco.cc/cancers/malt-lymphoma/), [Follicular lymphoma](https://onco.cc/cancers/follicular-lymphoma/), [Mantle cell lymphoma](https://onco.cc/cancers/mantle-cell-lymphoma/), [Marginal zone lymphoma](https://onco.cc/cancers/marginal-zone-lymphoma/), [Nodal marginal zone lymphoma](https://onco.cc/cancers/nodal-marginal-zone-lymphoma/), [Relapsed or refractory chronic lymphocytic leukaemia](https://onco.cc/cancers/cll-relapsed/), [Splenic marginal zone lymphoma](https://onco.cc/cancers/splenic-marginal-zone-lymphoma/), [Waldenström macroglobulinaemia](https://onco.cc/cancers/waldenstrom/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [BTK (Bruton tyrosine kinase)](https://onco.cc/targets/btk/)
- companies: [BeOne Medicines (formerly BeiGene)](https://onco.cc/companies/beone/)
- trials: [A Study of Emavusertib + An Approved Bruton Tyrosine Kinase Inhibitor (BTKi) in Participants With Chronic Lymphocytic Leukemia (CLL) and Other B-cell Malignancies](https://onco.cc/trials/nct07271667/), [A Study of GFH009 in Combination With Zanubrutinib in Subjects With Relapsed or Refractory DLBCL](https://onco.cc/trials/nct06375733/), [A Study of Zanubrutinib Plus Anti-CD20 Versus Lenalidomide Plus Rituximab in Participants With Relapsed/Refractory Follicular or Marginal Zone Lymphom](https://onco.cc/trials/nct05100862/), [A Study to Evaluate Long-term Safety of Zanubrutinib Regimens in Participants With B-Cell Malignancies Who Participated in BeiGene Parent Studies of Zanubrutinib](https://onco.cc/trials/nct04170283/), [A Study to Investigate Efficacy and Safety of BCL2 Inhibitor Sonrotoclax as Monotherapy and in Combination With Zanubrutinib in Adults With Waldenström Macroglobulinemia](https://onco.cc/trials/nct05952037/), [A Study to Investigate Safety and Effectiveness of Tacabrutideg (BGB-16673) in Combination With Other Agents in Participants With Relapsed or Refractory B-Cell Malignancies](https://onco.cc/trials/nct06634589/), [A Study to Investigate Sonrotoclax (BGB-11417) Plus Zanubrutinib (BGB-3111) Compared With Venetoclax Plus Acalabrutinib in Adults With Previously Untreated Chronic Lymphocytic Leukemia](https://onco.cc/trials/nct07277231/), [A Study to Investigate Sonrotoclax Combined With Zanubrutinib Versus Zanubrutinib Alone in Participants With Previously Untreated Chronic Lymphocytic Leukemia](https://onco.cc/trials/nct06637501/), [A Study to Investigate the Efficacy and Safety of Sonrotoclax Plus Zanubrutinib Compared With Placebo Plus Zanubrutinib in Adults With Relapsed/Refrac](https://onco.cc/trials/nct06742996/), [A Study to Investigate the Efficacy of Zanubrutinib Plus Rituximab Compared With Bendamustine Plus Rituximab in Adults With Previously Untreated Mantl](https://onco.cc/trials/nct04002297/), [A Study to Investigate the Safety of Novel Dose Ramp-up Schedule(s) When Initiating Sonrotoclax in Participants Treated for Blood Cancers.](https://onco.cc/trials/nct06697184/), [ALPINE](https://onco.cc/trials/alpine/), [ASPEN (Waldenström macroglobulinaemia)](https://onco.cc/trials/aspen-wm/), [CELESTIAL-TNCLL](https://onco.cc/trials/celestial-tncll/), [ROSEWOOD](https://onco.cc/trials/rosewood/), [SEQUOIA](https://onco.cc/trials/sequoia/), [Study of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)](https://onco.cc/trials/nct04662255/)
- terms: [BTK C481S, PLCG2 and BCL2 G101V resistance mutations](https://onco.cc/terms/btki-bcl2i-resistance-mutations/), [CLL-IPI (chronic lymphocytic leukaemia prognostic index)](https://onco.cc/terms/cll-ipi/), [MIPI (Mantle Cell Lymphoma International Prognostic Index)](https://onco.cc/terms/mipi/), [MYD88 L265P and CXCR4 mutations](https://onco.cc/terms/myd88-l265p/), [Richter transformation](https://onco.cc/terms/richter-transformation/), [Tyrosine kinase inhibitor (TKI)](https://onco.cc/terms/tki-term/), [What the NHS in England funds for lymphoma, appraisal by appraisal](https://onco.cc/terms/lymphoma-tx-uk-access/)
- pairings: [BTK inhibitor + venetoclax, fixed duration](https://onco.cc/pairings/btki-plus-venetoclax-fixed-duration/), [Caution: chemoimmunotherapy in del(17p)/TP53 CLL](https://onco.cc/pairings/cit-in-del17p-caution/), [Caution: ibrutinib in patients with cardiac risk](https://onco.cc/pairings/btki-ibrutinib-cardiac-caution/)
- ideas: [MRD-guided treatment duration in CLL](https://onco.cc/ideas/idea-mrd-guided-stop-cll/)
- biomarkers: [BTK resistance mutations: C481S, and L528W and T474I after the non-covalent inhibitors](https://onco.cc/biomarkers/btk-c481s/)
- key papers: [ELEVATE-TN: acalabrutinib, alone or with obinutuzumab, against chemo-immunotherapy in untreated CLL](https://onco.cc/key-papers/paper-elevate-tn-acalabrutinib-lancet-2020/), [MAGNOLIA: zanubrutinib in relapsed or refractory marginal zone lymphoma](https://onco.cc/key-papers/paper-magnolia-zanubrutinib-mzl-ccr-2021/), [ROSEWOOD: a phase II randomized study of zanubrutinib plus obinutuzumab versus obinutuzumab monotherapy in patients with relapsed or refractory follicular lymphoma](https://onco.cc/key-papers/paper-rosewood-zanubrutinib-obinutuzumab-follicular-jco-2023/)
- roadmaps: [Lymphoma roadmap: from a jaw tumour in Uganda and the first human cancer virus to gene-expression subtypes, PET-adapted chemotherapy, CAR-T cells, bispecific antibodies and the genetics-directed trials now recruiting](https://onco.cc/roadmaps/lymphoma-roadmap/)
- people: [John Oyler](https://onco.cc/people/oyler-john/)
- pathways: [Inflammation & NF-κB](https://onco.cc/pathways/inflammation-nfkb/)

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