Zanubrutinib Tablets Greenlit by FDA for All Approved Indications

Zanubrutinib has 5 approved indications in oncology.

An oral tablet formulation of zanubrutinib (Brukinsa) has received FDA approval for use in all approved indications of the Bruton tyrosine kinase (BTK) inhibitor, according to a press release from the drug’s developer, BeOne Medicines Ltd.¹

The tablets will contain 160 mg of zanubrutinib each, unlike the current 80-mg capsules. According to the release, the formulations have the same efficacy and safety profile, per 2 randomized single-dose, open-label phase 1 crossover studies of healthy adults conducted to establish bioequivalence. The tablets will also be smaller than the capsules and have a film coating.

Zanubrutinib tablets are set to replace the capsules in October 2025.

“[Zanubrutinib]’s leadership in the US underscores the trust physicians and patients have placed in its differentiated clinical profile,” said Matt Shaulis, general manager of BeOne, North America, in the press 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.”

The standard dosage of zanubrutinib, as a single agent or combined with obinutuzumab (Gazyva), is 320 mg taken either once daily or in two 160-mg doses, pending disease progression or unacceptable toxicity.²

Zanubrutinib Tablets and Liver Failure

Patients experiencing hepatic impairment may require a modified dose of zanubrutinib. Those with severe hepatic impairment should receive 160 mg of zanubrutinib daily via 80-mg doses administered orally twice daily. With the new tablets, this can be accomplished by splitting pills; when using capsules, patients should receive only 1 capsule at a time.

In cases where patients have mild or moderate hepatic impairment, they should receive the standard 320-mg dosage. Zanubrutinib is currently the sole BTK inhibitor with a recommended dosage for hepatic impairment.¹

Cancer Types Treated With Zanubrutinib

Zanubrutinib is a BTK inhibitor used in B-cell malignancies, currently approved for 5 indications in oncology.

The treatment was initially approved by the FDA in November 2019 for use in patients with mantle cell lymphoma (MCL) following at least 1 prior therapy. Zanubrutinib was then approved in September 2021 for use in Waldenström macroglobulinemia and for relapsed/refractory marginal zone lymphoma (MZL) after at least 1 or more CD20-targeted regimens.

Additionally, zanubrutinib received the OK for use in chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) in January 2023; following its initial approval, it was approved in the third-line setting for CLL/SLL when prior treatments included a BTK inhibitor and a BCL2 inhibitor.

Finally, the drug was granted accelerated approval in combination with obinutuzumab for patients with relapsed/refractory follicular lymphoma following at least 2 lines of systemic therapy. All indications are for adult patients.

Safety Profile

Zanubrutinib’s label contains warnings and precautions for hemorrhage, infections, cytopenias, second primary malignancies, cardiac arrhythmias, hepatotoxicity (including drug-induced liver injury), and embryo-fetal toxicity.

The most commonly reported adverse effects (AEs), as seen in at least 30% of patients, are neutropenia, thrombocytopenia, upper respiratory tract infection, hemorrhage, and musculoskeletal pain.

At the second occurrence of expected hematologic or nonhematologic AEs, a patient’s dosage should be reduced to 80 mg twice daily or 320 mg once daily following a drug holiday. At the fourth occurrence of such AEs, treatment with zanubrutinib should be discontinued.

Asymptomatic lymphocytosis occurring in patients with CLL or MCL should not be classified as an AE and should not cause treatment interruption or modification.

The European Medicines Agency is reviewing a marketing authorization application for the tablets, which is expected to be approved in 2025.

References

1. U.S. FDA approves tablet formulation of BeOne’s BRUKINSA for all approved indications. BeOne Medicines Ltd. News release. June 11, 2025. Accessed June 12, 2025. https://www.businesswire.com/news/home/20250611860939/en/U.S.-FDA-Approves-Tablet-Formulation-of-BeOnes-BRUKINSA-for-All-Approved-Indications
2. Zanubrutinib. Prescribing information. BeOne Medicines Ltd. November 14, 2019. Updated June 10, 2025. Accessed June 12, 2025. https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/218785Original2s000lbl.pdf