FDA Approves Tablet Formulation of Zanubrutinib for All Indications

The FDA has approved a new tablet formulation of zanubrutinib (Brukinsa; BeOne Medicines) for all approved indications, including patients with chronic lymphocytic leukemia (CLL); Waldenström's macroglobulinemia; mantle cell lymphoma after receiving at least 1 prior therapy; relapsed or refractory marginal zone lymphoma following at least 1 anti-CD20-based regimen; and relapsed or refractory follicular lymphoma in combination with obinutuzumab (Gazyva; Genentech) after 2 or more lines of systemic therapy, according to a news release from BeOne Medicines.^1,2

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Phase 1 Trials Indicate Bioequivalence Between Zanubrutinib Tablets and Capsules

Results from 2 single-dose, open-label, randomized phase 1 crossover studies of healthy adults served as the basis for this approval. These trials were designed to establish bioequivalence between zanubrutinib capsules and zanubrutinib tablets. The recommended dose for zanubrutinib remains at 320 mg daily; with the newly approved tablets being designed at 160 mg each, patients can take 2 tablets daily, compared with 4 of the currently available 80-mg capsules.¹

In addition, the tablets are smaller than zanubrutinib capsules and feature a film coating, making it easier for patients to swallow. As the only Bruton tyrosine kinase inhibitor (BTKi) to offer once or twice daily dosing, zanubrutinib's new form as a tablet stands to further improve patient quality of life when being treated with the medication. Zanubrutinib tablets are set to replace capsules beginning in October 2025, according to the news release.¹

“[Zanubrutinib's] leadership in the US underscores the trust physicians and patients have placed in its differentiated clinical profile,” Matt Shaulis, general manager of North America, BeOne, said in the news release. “With this new tablet formulation, we are making treatment simpler and more convenient—an important step forward for patients facing certain B-cell cancers.”¹

Proven Efficacy and Adverse Effect Considerations

Numerous clinical trials have established zanubrutinib's efficacy across its approved indications. Most recently, at the 2025 American Society of Clinical Oncology Meeting, 5-year follow-up data from the SEQUOIA study was presented, indicating that zanubrutinib elicits meaningful 60-month progression-free survival of approximately 72.2% in patients with CLL. Furthermore, zanubrutinib demonstrated a clinically meaningful overall response rate of 97.3%.³

Although the efficacy of zanubrutinib is clear, there are some key risks of BTKis that pharmacists and health care providers must be aware of. Agents such as ibrutinib (Imbruvica; Janssen Biotech) can increase the risk of stroke in patients with atrial fibrillation (AF) by up to 30%, making second- and third-generation agents such as zanubrutinib or acalabrutinib (Calquence; AstraZeneca) preferred in treatment; however, these agents have not been evaluated in head-to-head trials.⁴

Pharmacists stand to play an essential role once new zanubrutinib tablets enter the market. They must counsel patients on the proven efficacy of the tablets compared with the capsules and assure them that the effects of their treatment will not be diminished. Additionally, because the tablets come in smaller doses than the capsules, patients must be educated on proper dosing and administration with zanubrutinib. Adverse effects should also be continuously monitored, especially in patients with AF.

REFERENCES

1. BeOne Medicines Ltd. U.S. FDA approves tablet formulation of BeOne's BRUKINSA for all approved indications. News Release. Released June 11, 2025. Accessed June 11, 2025. https://www.businesswire.com/news/home/20250611860939/en/U.S.-FDA-Approves-Tablet-Formulation-of-BeOnes-BRUKINSA-for-All-Approved-Indications

2. BRUKINSA. Package insert. BeiGene USA, Inc.; 2025. Accessed June 11, 2025. chrome-extension://efaidnbmnnnibpcajpcglclefindmkaj/https://d1e94vsyskgtht.cloudfront.net/brukinsa/pdfs/brukinsa-prescribing-information.pdf

3. Gerlach A. Five-year follow-up data show zanubrutinib improves progression-free survival, overall survival in CLL/SLL. Pharmacy Times. Published May 27, 2025. Accessed June 12, 2025. https://www.pharmacytimes.com/view/five-year-follow-up-data-shows-zanubrutinib-improves-progression-free-survival-overall-survival-in-cll-sll

4. Gerlach A, Spinler S. Cardiovascular risks of BTK inhibitors: What pharmacists need to know. Pharmacy Times. Published April 1, 2025. Accessed June 12, 2025. https://www.pharmacytimes.com/view/cardiovascular-risks-of-btk-inhibitors-what-pharmacists-need-to-know