Brukinsa

Mantle cell lymphoma (MCL) in adults who have received at least one prior therapy; Waldenström's macroglobulinemia (WM); Marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen; Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)

Standard dose: 160 mg orally twice daily or 320 mg once daily
Swallow capsules whole with or without food
CYP3A strong inhibitors: Reduce to 80 mg once daily
CYP3A moderate inhibitors: Reduce to 80 mg twice daily
Missed dose: Take as soon as possible on the same day; do not double dose

Capsules: 80 mg

None listed.

• Hemorrhage: Fatal and serious hemorrhagic events reported (4.3% serious). Use caution with anticoagulants/antiplatelets. Withhold 3-7 days pre/post-surgery.
• Infections: Fatal and serious infections (including COVID-19 pneumonia, pneumonia, sepsis). Monitor and treat promptly. Consider prophylaxis for herpes virus, Pneumocystis jirovecii, and other infections.
• Cytopenias: Grade 3-4 neutropenia (23%), thrombocytopenia (8%), anemia (8%). Monitor CBC monthly.
• Second Primary Malignancies: Reported in 14% of patients including non-melanoma skin cancers.
• Cardiac Arrhythmias: Atrial fibrillation/flutter reported in 4.4%. Monitor patients with risk factors.
• Embryo-Fetal Toxicity

Neutropenia (30%), upper respiratory tract infection (24%), hemorrhage/bruising (22%), musculoskeletal pain (20%), rash (17%), diarrhea (15%), cough (14%), fatigue (13%), pneumonia (12%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Zanubrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK). It forms a covalent bond with a cysteine residue (C481) in the BTK active site, leading to sustained inhibition of BTK enzymatic activity. BTK is a signaling molecule in the B-cell receptor (BCR) pathway; its inhibition reduces malignant B-cell proliferation, trafficking, chemotaxis, and adhesion.

Median Tmax: 2 hours. Steady-state AUC increased dose-proportionally. Half-life: approximately 2-4 hours. Metabolized primarily by CYP3A. Excreted in feces (87%) and urine (8%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• ALPINE — Zanubrutinib vs. ibrutinib in relapsed/refractory CLL/SLL. Phase III, n=652.
  🔬 NCT03734016 ↗ 📄 Primary Publication ↗

Brukinsa has FDA-approved indications across the following cancer types covered on PipelineEvidence: