FDA Approves New Tablet Formulation of BRUKINSA for All Indications, Reducing Pill Burden for B-Cell Cancer Patients
Key Insights
The U.S. FDA has approved a new tablet formulation of BRUKINSA (zanubrutinib) for all five approved indications, reducing daily pill burden from four capsules to two tablets while maintaining the same 320 mg daily dose.
The new 160 mg tablets demonstrate bioequivalence to the existing capsules based on Phase 1 crossover studies and offer improved patient convenience with smaller size and film coating for easier swallowing.
BRUKINSA has achieved market leadership as the top BTK (search) inhibitor in the U.S. and leads in new chronic lymphocytic leukemia (search) patient starts across all therapy lines.
The U.S. Food and Drug Administration has approved a new tablet formulation of BRUKINSA® (zanubrutinib) for all five approved indications, marking a significant advancement in patient convenience for those with B-cell malignancies. BeOne Medicines (search) Ltd. announced the approval on June 11, 2025, highlighting that the new formulation reduces pill burden while maintaining therapeutic efficacy.
Simplified Dosing Regimen
The new BRUKINSA tablets are 160 mg each, allowing patients to take two tablets daily instead of four 80 mg capsules, while maintaining the recommended 320 mg daily dose. The tablets are smaller than the current capsules and feature a film coating designed to make them easier to swallow.
"With this new tablet formulation, we are making treatment simpler and more convenient—an important step forward for patients facing certain B-cell cancers," said Matt Shaulis, General Manager of North America at BeOne.
Bioequivalence Established
The tablet formulation demonstrates the same efficacy and safety profile as the capsule form, based on results from two single-dose, open-label, randomized Phase 1 crossover studies conducted in healthy adults. These studies were specifically designed to establish bioequivalence between the formulations.
BRUKINSA maintains its unique position as the only BTK (search) inhibitor offering flexible once or twice daily dosing options, allowing physicians to tailor treatment schedules to individual patient needs. It also remains the only BTK inhibitor with recommended dosing guidelines for patients with severe hepatic impairment.
Market Leadership Position
BRUKINSA has achieved significant market penetration, becoming the overall BTK (search) inhibitor market share leader for the first time while maintaining its position as the leader in new chronic lymphocytic leukemia (search) (CLL) patient starts across all lines of therapy in the U.S.
The drug's clinical profile has established trust among physicians and patients, according to company leadership. BRUKINSA is distinguished as the only BTK (search) inhibitor to demonstrate superiority over another BTK inhibitor in a Phase 3 study.
Global Clinical Program and Approvals
The global BRUKINSA clinical development program encompasses approximately 7,100 patients enrolled across 30 countries and regions in more than 35 trials. The drug has received approval in more than 75 markets for at least one indication, with over 200,000 patients treated globally.
Approved Indications
BRUKINSA is approved for 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 operate under accelerated approval based on overall response rate and durability of response, with continued approval contingent upon verification of clinical benefit in confirmatory trials.
Safety Profile
The most common adverse reactions (≥30%) in patients receiving BRUKINSA include decreased neutrophil count (51%), decreased platelet count (41%), upper respiratory tract infection (38%), hemorrhage (32%), and musculoskeletal pain (31%) based on data from 1,729 patients.
Grade 3 or higher hemorrhage occurred in 3.8% of patients, with fatalities in 0.2% of cases. Grade 3 or higher infections occurred in 26% of patients, most commonly pneumonia (7.9%), with fatal infections in 3.2% of patients.
Implementation Timeline
The BRUKINSA tablets will replace capsules beginning in October 2025. The European Medicines Agency is currently reviewing a Type II variation marketing authorization application for the new tablet formulation across all currently approved indications, with approval anticipated later this year.
Mechanism of Action
BRUKINSA is an orally available, small molecule inhibitor of Bruton's tyrosine kinase (search) (BTK (search)) designed to deliver complete and sustained inhibition of the BTK protein through optimized bioavailability, half-life, and selectivity. The drug has demonstrated ability to inhibit proliferation of malignant B cells within disease-relevant tissues, with differentiated pharmacokinetics compared to other approved BTK inhibitors.