UNMATCHED BTKi
DOSING FLEXIBILITY1-3

BRUKINSA® (zanubrutinib) dosing options

ADDITIONAL FLEXIBILITY: STRAIGHTFORWARD DOSE MODIFICATIONS
WITHOUT EXCHANGES1

Two pills side-by-side

Straightforward dose modification

  • Simply reduce the number of BRUKINSA capsules
    1. Ability to reduce the dose in small increments
    2. Rates of dose reductions (0.8%-11%) were low across BRUKINSA studies
Pill bottle with pill

No dose exchanges needed

  • BRUKINSA does not require a new prescription or dose exchange for dose reductions
  • Can be taken with or without food. Can be taken with a high-fat meal—BRUKINSA drug concentration (AUC) is not affected
  • Advise patients to swallow capsules whole with water—do not open, break, or chew capsules
  • If a dose of BRUKINSA is missed, it should be taken as soon as possible with a return to the normal schedule the following day

BRUKINSA should be taken until disease progression or unacceptable toxicity.

AUC=area under the concentration-time curve; BTKi=Bruton’s tyrosine kinase inhibitor.

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NO DOSE ADJUSTMENTS REQUIRED WITH THESE COMMON MEDICATIONS

Stomach icon Gastric Acid Reducing Agents1

Proton pump inhibitors

Including, but not limited to:

  • Omeprazole
  • Esomeprazole
  • Lansoprazole

H2-receptor antagonists

Including, but not limited to:

  • Famotidine
  • Ranitidine
  • Nizatidine
Red blood cells icon Anticlotting Medication1,4

Anticoagulants

  • Heparins
  • Direct thrombin inhibitors
  • Factor Xa inhibitors
  • Vitamin K antagonists

Antiplatelets

  • Aspirin
  • P2Y12 inhibitors
  • Phosphodiesterase inhibitors
  • PAR-1 antagonists

BRUKINSA was allowed to be coadministered in clinical trials with antiplatelets and anticoagulants (as long as INR was ≤1.5 and aPTT ≤1.5 x ULN).4-6

Coadministration of BRUKINSA with antiplatelet or anticoagulant medications may increase the risk of hemorrhage. Monitor for signs and symptoms of bleeding.1

WITH BRUKINSA, DOSE MODIFICATIONS ARE AS STRAIGHTFORWARD AS REDUCING THE NUMBER OF PILLS, WITH THE ABILITY TO DOSE REDUCE IN SMALL INCREMENTS1

Grade ≥3 events requiring dose modifications

  • Grade 3 or Grade 4 febrile neutropenia
  • Platelet count decreased to 25,000-50,000/mm3 with significant bleeding
  • Neutrophil count decreased to <500/mm3*
  • Platelet count decreased to <25,000/mm3*
  • Severe or life-threatening non-hematological toxicities†
BRUKINSA® (zanubrutinib) dose reductions

*Lasting more than 10 consecutive days.

†Evaluate the benefit-risk before resuming treatment at the same dosage for Grade 4 non-hematological toxicity.

aPTT=activated partial thromboplastin time; INR=International Normalized Ratio; PAR-1=protease-activated receptor 1; ULN=upper limit of normal.

Asymptomatic lymphocytosis should not be regarded as an adverse reaction, and these patients should continue taking BRUKINSA.

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IMPORTANT SAFETY INFORMATION

WARNINGS AND PRECAUTIONS

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. Consider the benefit-risk of withholding BRUKINSA for 3-7 days before and after surgery depending upon the type of surgery and the risk of bleeding.

Infections

Fatal and serious infections (including bacterial, viral, or fungal infections) and opportunistic infections have occurred in patients with hematological malignancies treated with BRUKINSA. Grade 3 or higher infections occurred in 26% of patients, most commonly pneumonia (7.9%), with fatal infections occurring in 3.2% of patients. Infections due to hepatitis B virus (HBV) reactivation have occurred.

Consider prophylaxis for herpes simplex virus, pneumocystis jirovecii pneumonia, and other infections according to standard of care in patients who are at increased risk for infections. Monitor and evaluate patients for fever or other signs and symptoms of infection and treat appropriately.

Cytopenias

Grade 3 or 4 cytopenias, including neutropenia (21%), thrombocytopenia (8%) and anemia (8%) based on laboratory measurements, developed in patients treated with BRUKINSA. Grade 4 neutropenia occurred in 10% of patients, and Grade 4 thrombocytopenia occurred in 2.5% of patients.

Monitor complete blood counts regularly during treatment and interrupt treatment, reduce the dose, or discontinue treatment as warranted. Treat using growth factor or transfusions, as needed.

Second Primary Malignancies

Second primary malignancies, including non-skin carcinoma, have occurred in 14% of patients treated with BRUKINSA. The most frequent second primary malignancy was non-melanoma skin cancers (8%), followed by other solid tumors in 7% of the patients (including melanoma in 1% of patients) and hematologic malignancies (0.7%). Advise patients to use sun protection and monitor patients for the development of second primary malignancies.

Cardiac Arrhythmias

Serious cardiac arrhythmias have occurred in patients treated with BRUKINSA. Atrial fibrillation and atrial flutter were reported in 4.4% of patients treated with BRUKINSA, including Grade 3 or higher cases in 1.9% of patients. Patients with cardiac risk factors, hypertension, and acute infections may be at increased risk. Grade 3 or higher ventricular arrhythmias were reported in 0.3% of patients.

Monitor for signs and symptoms of cardiac arrhythmias (e.g., palpitations, dizziness, syncope, dyspnea, chest discomfort), manage appropriately, and consider the risks and benefits of continued BRUKINSA treatment.

Hepatotoxicity, Including Drug-Induced Liver Injury

Hepatotoxicity, including severe, life-threatening, and potentially fatal cases of drug-induced liver injury (DILI), has occurred in patients treated with Bruton tyrosine kinase inhibitors, including BRUKINSA.

Evaluate bilirubin and transaminases at baseline and throughout treatment with BRUKINSA. For patients who develop abnormal liver tests after BRUKINSA, monitor more frequently for liver test abnormalities and clinical signs and symptoms of hepatic toxicity. If DILI is suspected, withhold BRUKINSA. Upon confirmation of DILI, discontinue BRUKINSA.

Embryo-Fetal Toxicity

Based on findings in animals, BRUKINSA can cause fetal harm when administered to a pregnant woman. Administration of zanubrutinib to pregnant rats during the period of organogenesis caused embryo-fetal toxicity, including malformations at exposures that were 5 times higher than those reported in patients at the recommended dose of 160 mg twice daily. Advise women to avoid becoming pregnant while taking BRUKINSA and for 1 week after the last dose. Advise men to avoid fathering a child during treatment and for 1 week after the last dose. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.

ADVERSE REACTIONS

The most common adverse reactions (≥30%), including laboratory abnormalities, in patients who received BRUKINSA (N=1729) are decreased neutrophil count (51%), decreased platelet count (41%), upper respiratory tract infection (38%), hemorrhage (32%), and musculoskeletal pain (31%).

DRUG INTERACTIONS

CYP3A Inhibitors: When BRUKINSA is coadministered with a strong CYP3A inhibitor, reduce BRUKINSA dose to 80 mg once daily. For coadministration with a moderate CYP3A inhibitor, reduce BRUKINSA dose to 80 mg twice daily.

CYP3A Inducers: Avoid coadministration with strong or moderate CYP3A inducers. Dose adjustment may be recommended with moderate CYP3A inducers.

SPECIFIC POPULATIONS

Hepatic Impairment: The recommended dose of BRUKINSA for patients with severe hepatic impairment is 80 mg orally twice daily.

INDICATIONS

BRUKINSA is a kinase inhibitor indicated for the treatment of adult patients with:

  • Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)
  • Waldenström’s macroglobulinemia (WM)
  • Mantle cell lymphoma (MCL) who have received at least one prior therapy
  • Relapsed or refractory marginal zone lymphoma (MZL) who have received at least one anti-CD20-based regimen
  • Relapsed or refractory follicular lymphoma (FL), in combination with obinutuzumab, after two or more lines of systemic therapy

The MCL, MZL and FL indications are approved under accelerated approval based on overall response rate and durability of response. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials.

Please see full Prescribing Information.

References: 1. BRUKINSA. Package insert. BeiGene USA, Inc.; 2025. 2. CALQUENCE. Package insert. AstraZeneca Pharmaceuticals LP; 2025. 3. IMBRUVICA. Package insert. Pharmacyclics LLC, Janssen Biotech, Inc; 2024. 4. Tam CS, Opat S, Zhu J, et al. Pooled analysis of safety data from monotherapy studies of the Bruton tyrosine kinase (BTK) inhibitor, zanubrutinib (BGB-3111) in B-cell malignancies. Poster presented at: European Hematology Association (EHA) 2019 Annual Meeting; June 13-16, 2019. Abstract PS1159. 5. Data on file. BeiGene USA, Inc. 6. BeiGene. Study of the safety and pharmacokinetics of BGB-3111 in subjects with B-cell lymphoid malignancies. ClinicalTrials.gov website. NCT02343120. Last updated April 28, 2022. Accessed February 7, 2025. https://clinicaltrials.gov/ct2/show/NCT02343120