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zanubrutinib (Brukinsa)
Indications:
- mantle cell lymphoma
- Waldenstrom's macroglobulinemia [3]
- first line treatment of chronic lymphocytic leukemia & small lymphocytic lymphoma in older patients (> 65 years) [4]
Dosage:
- 160 mg PO BID or 320 mg PO QD
Capsule: 80 mg
Pharmacokinetics:
- metabolized by CYP3A
- eliminated in feces (38% unchanged) & 8% in urine (< 1% unchanged)
Adverse effects:
- leukopenia, neutropenia, thrombocytopenia, anemia
- rash, bruising, diarrhea, cough
- serious: pneumonia (11%), hemorrhage (5%)
Drug interactions:
- CYP3A inhibitors: modify dose
- avoid with moderate or strong CYP3A inducers
Mechanism of action:
- selective Bruton tyrosine kinase inhibitor [4]
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid=135565884
References
- RxNorm
- FDA Drug Approval, Nov 14, 2019
FDA grants accelerated approval to zanubrutinib for mantle cell lymphoma.
https://www.fda.gov/drugs/resources-information-approved-drugs/fda-grants-accelerated-approval-zanubrutinib-mantle-cell-lymphoma
- FDA Drug Approval. Aug 31, 2021
FDA approves zanubrutinib for Waldenstrom's macroglobulinemia.
https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-zanubrutinib-waldenstroms-macroglobulinemia
- Bassett M
Zanubrutinib Wins in First-Line CLL for Older Patients.
The BTK inhibitor proves superior to bendamustine-rituximab in phase III trial.
MedPage Today July 8, 2022
https://www.medpagetoday.com/hematologyoncology/leukemia/99653
- Tam CS, Brown JR, Kahl BS et al
Zanubrutinib versus bendamustine and rituximab in untreated chronic
lymphocytic leukaemia and small lymphocytic lymphoma (SEQUOIA):
a randomised, controlled, phase 3 trial.
Lancet Oncology. 2022. July 7.
PMID: 35810754
https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(22)00293-5/fulltext
- Highlights of Prescribing Information.
BRUKINSA (zanubrutinib) capsules, for oral use
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/213217s000lbl.pdf