Brukinsa Zanubrutinib

1. ‌Indications and Usage‌
Mantle Cell Lymphoma (MCL): Suitable for adult patients who have received at least one therapy in the past.
Waldenstr ö m’s Macroglobulin (WM): Used as a monotherapy for the treatment of adult patients.
Relapsed or Refractory Marginal Zone Lymphoma (MZL): Suitable for patients who have received at least one anti-CD20 regimen treatment.
In the above indications, the approval of MCL and WM is based on overall response rate (ORR), and continued approval depends on the validation of clinical benefits by confirmatory trials.
2. ‌Dosage and Administration‌
Recommended dosage:
MCL, WM, MZL: 160 mg orally, twice daily, or 320 mg orally, once daily.
Dosage form and specifications: Capsules (80 mg, 160 mg); Tablets (160 mg).
Dose adjustment:
When combined with potent CYP3A inhibitors such as ketoconazole, the dose should be halved (i.e. 80 mg twice daily or 160 mg once daily).
Patients with severe liver function impairment: The recommended dose is 80 mg twice daily.
When a toxic reaction of grade ≥ 3 occurs, medication can be temporarily suspended and restarted at the original dose or reduced dosage after recovery.
3. ‌Mechanism of Action‌

Zanubrutinib is a covalent, irreversible Bruton tyrosine kinase (BTK) inhibitor that selectively blocks the B cell receptor signaling pathway, inhibits B cell proliferation and survival, and exerts anti-tumor effects in B cell malignancies.

4. ‌Safety and Warnings‌
Bleeding risk: Serious bleeding events (including intracranial hemorrhage) have been reported, and medication discontinuation strategies before and after surgery need to be evaluated.
Infection: Common bacterial, viral, or fungal infections, including pneumonia and reactivation of shingles.
Arrhythmia: including atrial fibrillation and atrial flutter, especially in patients with a history of cardiovascular disease, heart rate monitoring is necessary.
Second primary malignant tumor: an increased incidence of skin cancer and other solid tumors has been observed.
Embryo fetal toxicity: can cause fetal damage, it is recommended that women of childbearing age take effective contraceptive measures during treatment and at least 6 months after the last dose.
5. ‌Adverse Reactions‌
Common adverse reactions (≥ 20%): neutropenia, thrombocytopenia, rash, bruising, diarrhea, upper respiratory tract infection.
Grade 3 or above adverse reactions: neutropenia (18.6%), infectious pneumonia (7.0%), thrombocytopenia (4.7%), etc.
The incidence of serious adverse reactions is about 15.1%, with infectious pneumonia being the most common (8.1%).
6. ‌Drug Interactions‌
CYP3A inhibitors/inducers: significantly affect blood drug concentration. Avoid co administration with potent CYP3A inhibitors (such as itraconazole) or inducers (such as rifampicin); If combined use is necessary, the dosage needs to be adjusted.
Anticoagulants or antiplatelet drugs: Co administration may increase the risk of bleeding and should be monitored with caution.
7. ‌Pharmaceutical Information‌
Product Name: BRUKINSA ®
Common name: Zanubrutinib
R&D company: BeiGene
FDA approval date: First approved in November 2019 (MCL), with subsequent extended indications approved gradually
Storage conditions: Room temperature (20-25 ° C), away from light and moisture