Zanubrutinib

Zanubrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK). Zanubrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK activity.

• BRUKINSA is a kinase inhibitor indicated for the treatment of adult patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy. ( 1.1 ) This indication is approved under accelerated approval based on overall response rate.ICD-10: C85.90

• None. None.contraindicated

Recommended dosage: 160 mg orally twice daily or 320 mg orally once daily with or without food; swallow whole with water. Tablets can be split in half as prescribed by the healthcare provider. ( 2.1 ) Reduce BRUKINSA dose in patients with severe hepatic impairment. ( 2.2 , 8.7 ) Advise patients not to open, break, or chew capsules. ( 2.1 ) Advise patients not to chew or crush tablets. ( 2.1 ) Manage toxicity using treatment interruption, dose reduction, or discontinuation. ( 2.4 ) 2.1 Recommended Dosage The recommended dosage of BRUKINSA for monotherapy or in combination with obinutuzumab is 160 mg taken orally twice daily or 320 mg taken orally once daily until disease progression or unacceptable toxicity. Capsule Administration Instructions Administer BRUKINSA capsules with or without food [see Clinical Pharmacology (12.3) ] . Advise patients to swallow capsules whole with water and not to open, break, or chew capsules. Tablet Administration Instructions Administer BRUKINSA tablets with or without food [see Clinical Pharmacology (12.3) ] . Advise patients to swallow tablets whole with water and not to chew or crush the tablets. The tablets can be split in half as prescribed by the healthcare provider. Missed Dose If a dose of BRUKINSA is missed, it should be taken as soon as possible on the same day with a return to the normal schedule the following day.

Hemorrhage : Monitor for bleeding and manage appropriately. ( 5.1 ) Infections : Monitor patients for signs and symptoms of infection, including opportunistic infections, and treat as needed. ( 5.2 ) Cytopenias : Monitor complete blood counts during treatment. ( 5.3 ) Second Primary Malignancies : Other malignancies have developed including skin cancers and non-skin carcinomas. Monitor and advise patients to use sun protection. ( 5.4 ) Cardiac Arrhythmias : Monitor for signs and symptoms of arrhythmias and manage appropriately. ( 5.5 ) Hepatotoxicity, Including Drug-Induced Liver Injury : Monitor hepatic function throughout treatment. ( 5.6 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise women of the potential risk to a fetus and to use effective contraception. ( 5.7 ) 5.1 Hemorrhage Fatal and serious hemorrhage has occurred in patients with hematological malignancies treated with BRUKINSA. Grade 3 or higher hemorrhage including intracranial and gastrointestinal hemorrhage, hematuria, and hemothorax was reported in 3.8% of patients treated with BRUKINSA in clinical trials, with fatalities occurring in 0.2% of patients. Bleeding of any grade, excluding purpura and petechiae, occurred in 32% of patients. Bleeding has occurred in patients with and without concomitant antiplatelet or anticoagulation therapy. Coadministration of BRUKINSA with antiplatelet or anticoagulant medications may further increase the risk of hemorrhage. Monitor for signs and symptoms of bleeding. Discontinue BRUKINSA if intracranial hemorrhage of any grade occurs.

The following clinically significant adverse reactions are discussed in more detail in other sections of the labeling: Hemorrhage [see Warnings and Precautions (5.1) ] Infections [see Warnings and Precautions (5.2) ] Cytopenias [see Warnings and Precautions (5.3) ] Second Primary Malignancies [see Warnings and Precautions (5.4) ] Cardiac Arrhythmias [see Warnings and Precautions (5.5) ] Hepatotoxicity, including DILI [see Warnings and Precautions (5.6) ] The most common adverse reactions (≥30%), including laboratory abnormalities, are neutrophil count decreased, platelet count decreased, upper respiratory tract infection, hemorrhage, and musculoskeletal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact BeOne Medicines at 1-877-828-5596 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data in the WARNINGS AND PRECAUTIONS reflect exposure to BRUKINSA in nine monotherapy and 2 combination clinical trials, administered at 160 mg twice daily in 1608 patients and at 320 mg once daily in 121 patients. Among these 1729 patients, the median duration of exposure was 27.6 months, 78% of patients were exposed for at least 12 months, and 60% of patients were exposed for at least 24 months.

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings in animals, BRUKINSA can cause fetal harm when administered to pregnant women. There are no available data on BRUKINSA use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of zanubrutinib to pregnant rats during the period of organogenesis was associated with fetal heart malformation at approximately 5-fold human exposures (see Data ) . Women should be advised to avoid pregnancy while taking BRUKINSA. If BRUKINSA is used during pregnancy, or if the patient becomes pregnant while taking BRUKINSA, the patient should be apprised of the potential hazard to the fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Embryo-fetal development toxicity studies were conducted in both rats and rabbits.

Metabolism

Zanubrutinib maximum plasma concentration (C max ) and area under the plasma drug concentration over time curve (AUC) increase proportionally over a dosage range from 40 mg to 320 mg (0.13 to 1 time the recommended total daily dose). Limited systemic accumulation of zanubrutinib was observed following repeated administration.

• Nov 14, 2019NDANDA213217Beone Medicines Usa
• Jun 10, 2025NDANDA218785Beone Medicines Usa

1. 1Off Label Use51814%
2. 2Disease Progression2737.1%
3. 3White Blood Cell Count Decreased2275.9%
4. 4Myelosuppression2215.8%
5. 5Anaemia2155.6%
6. 6Platelet Count Decreased2085.4%
7. 7Contusion2065.4%
8. 8Fatigue1975.1%
9. 9Rash1854.8%
10. 10Pneumonia1704.4%
11. 11Death1674.4%
12. 12Diarrhoea1544.0%
13. 13Asthenia1423.7%
14. 14Neutrophil Count Decreased1393.6%
15. 15Drug Ineffective1283.3%

The 10 most recently updated of 223 ClinicalTrials.gov registrations naming Zanubrutinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Emavusertib + An Approved Bruton Tyrosine Kinase Inhibitor (BTKi) in Participants With Chronic Lymphocytic Leukemia (CLL) and Other B-cell Malignancies
  Recruiting · Phase 2 · Interventional · 108 enrolled · Curis, Inc.
  NCT07271667updated 2026-06-12
• A Study of Nemtabrutinib (MK-1026) in Participants With Relapsed or Refractory Hematologic Malignancies (ARQ 531-101/MK-1026-001)
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 190 enrolled · ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)
  NCT03162536updated 2026-06-12
• Testing the Combination of Venetoclax and Rituximab, in Comparison to the Usual Treatment (Ibrutinib Plus Rituximab or Zanubrutinib Alone) for Waldenstrom's Macroglobulinemia/Lymphoplasmacytic Lymphoma
  Recruiting · Phase 2 · Interventional · 92 enrolled · National Cancer Institute (NCI)
  NCT04840602updated 2026-06-11
• Zanubritnib and Anti-MAG Neuropathy
  Recruiting · Phase 2 · Interventional · 50 enrolled · Azienda Ospedaliera di Padova
  NCT07392229updated 2026-06-10
• A Study of Zanubrutinib Plus Anti-CD20 Versus Lenalidomide Plus Rituximab in Participants With Relapsed/Refractory Follicular or Marginal Zone Lymphoma
  Recruiting · Phase 3 · Interventional · 780 enrolled · BeOne Medicines
  NCT05100862updated 2026-06-10
• Testing Mosunetuzumab Alone, With Zanubrutinib, or With Polatuzumab Vedotin for Treating Marginal Zone Lymphoma That Came Back or Didn't Get Better With Treatment
  Not yet recruiting · Phase 2 · Interventional · 138 enrolled · SWOG Cancer Research Network
  NCT07638722updated 2026-06-10
• A Study to Evaluate Zanubrutinib and Tislelizumab in Progressive Lymphoma Post CAR-T
  Recruiting · Phase 2 · Interventional · 76 enrolled · University Health Network, Toronto
  NCT06167785updated 2026-06-09
• Zanubrutinib, Bendamustine, Rituximab Prev. Untreated WM
  Recruiting · Phase 2 · Interventional · 56 enrolled · Massachusetts General Hospital
  NCT06561347updated 2026-06-08
• A Study to Investigate the Safety of Novel Dose Ramp-up Schedule(s) When Initiating Sonrotoclax in Participants Treated for Blood Cancers.
  Recruiting · Phase 1 · Phase 2 · Interventional · 258 enrolled · BeOne Medicines
  NCT06697184updated 2026-06-08
• Zanubrutinib in Combination With R-PolaCHP (ZaR-PolaCHP) for Newly Diagnosed Diffuse Large B-Cell Lymphoma
  Suspended · Phase 1 · Interventional · 38 enrolled · Yazeed Sawalha
  NCT04850495updated 2026-06-04

Frequently asked questions

How does Zanubrutinib work?

Zanubrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK). Zanubrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK activity.

What is Zanubrutinib used for?

According to FDA labeling, Zanubrutinib carries indications including: BRUKINSA is a kinase inhibitor indicated for the treatment of adult patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy. ( 1.1 ) This indication is approved under accelerated approval based on overall response rate.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Zanubrutinib?

Zanubrutinib is classified as Bruton's tyrosine kinase (BTK) inhibitors, Kinase Inhibitor, Bruton's Tyrosine Kinase Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Zanubrutinib?

Zanubrutinib is marketed under brand names including Brukinsa.

What are the contraindications for Zanubrutinib?

Zanubrutinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.