FDA Approves Zanubrutinib Tablet for All Indications
The FDA has approved a tablet version of zanubrutinib for all indications, improving convenience and reducing pill burden for patients with blood cancers.
US FDA
The FDA has approved a new tablet formulation of zanubrutinib (Brukinsa), a Bruton tyrosine kinase (BTK) inhibitor, for all 5 of its previously approved indications.1
This development is anticipated to streamline administration and enhance patient convenience by reducing pill burden. The new tablet form is expected to be available for prescription by 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 North America, BeOne Medicines, in a 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.”
Zanubrutinib is indicated for the treatment of adult patients with:
- Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)
- Waldenström macroglobulinemia (WM)
- Mantle cell lymphoma (MCL) who have received at least 1 prior therapy
- Relapsed or refractory marginal zone lymphoma (MZL) who have received at least 1 anti-CD20–based regimen
- Relapsed or refractory follicular lymphoma (FL), in combination with obinutuzumab (Gazvya), after 2 or more lines of systemic therapy.
The approval of the tablet formulation was based on data from 2 single-dose, open-label, randomized phase 1 crossover studies in healthy adults. These studies demonstrated bioequivalence between the new tablet and the existing capsule formulation of zanubrutinib. The recommended dosage remains 320 mg daily, which can now be achieved with 2 160 mg tablets, reducing the previous requirement of 4 80 mg capsules. This reduction in pill count, coupled with the smaller size and film coating of the tablets, is intended to improve ease of swallowing and overall patient adherence to therapy.
Chronic lymphocytic leukemia cells: © Mari-stocker - stock.adobe.com
Zanubrutinib has established itself as a leading BTK inhibitor, recognized for its differentiated pharmacokinetic profile and efficacy across various B-cell malignancies. It is currently the only BTK inhibitor offering both once- or twice-daily dosing flexibility and recommended dosing for severe hepatic impairment. Clinical trials supporting its original approvals have enrolled approximately 7100 patients across more than 35 trials in 30 countries and regions. Globally, zanubrutinib is approved in over 75 markets, with more than 200,000 patients having received treatment.
The transition to a tablet formulation addresses a common challenge in chronic oncology care: medication adherence. Simplifying dosing regimens can contribute to improved treatment consistency and, potentially, better long-term outcomes for patients with these hematologic malignancies.
Clinicians should continue to monitor patients for known adverse events associated with zanubrutinib, including hemorrhage, infections, cytopenias, second primary malignancies, and cardiac arrhythmias, as detailed in the prescribing information. The safety profile of the new tablet formulation is expected to be consistent with the capsule.2
The European Medicines Agency is also reviewing a Type II variation marketing authorization application for the zanubrutinib tablet formulation for all 5 indications, with a decision expected later this year.1
