Currently Enrolling Trials
Brukinsa (zanubrutinib) is a kinase inhibitor.
Brukinsa is specifically indicated for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.
Brukinsa is supplied as a capsule for oral administration. The recommended dose is 160 mg taken orally twice daily or 320 mg taken orally once daily until disease progression or unacceptable toxicity. Brukinsa can be taken with or without food. Capsules should be swallowed whole with water. Capsules should not be opened, broken or chewed. If a dose of Brukinsa is missed, it should be taken as soon as possible on the same day with a return to the normal schedule the following day.
Mechanism of Action
Brukinsa (zanubrutinib) is a small-molecule inhibitor of BTK. Zanubrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. In B-cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion.
Adverse effects associated with the use of Brukinsa may include, but are not limited to, the following:
- neutrophil count decreased
- platelet count decreased
- upper respiratory tract infection
- white blood cell count decreased
- hemoglobin decreased
Clinical Trial Results
Brukinsa was approved under accelerated approval based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
A single-arm clinical trial of Brukinsa included 86 patients with mantle cell lymphoma who had received at least one prior treatment. The trial measured how many patients experienced complete or partial shrinkage of their tumors after treatment (overall response rate). In the trial, 84% of patients had tumor shrinkage with a median duration of response (time between the initial response to therapy and subsequent disease progression or relapse) of 19.5 months. This trial was supported by an additional single-arm trial that included 32 patients, in which 84% of patients had tumor shrinkage with a median duration of response of 18.5 months.