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BTK Inhibitor Pregnancy: Contraindicated — embryotoxic in animal studies; effective contraception required during and for 1 week after

Zanubrutinib

Brand names: Brukinsa

Adult dose

Dose: 160 mg twice daily or 320 mg once daily
Route: Oral
Frequency: Twice daily or once daily
Max: 320 mg/day
CLL/SLL, MCL, Waldenström's; continue until progression or unacceptable toxicity; no food restriction

Paediatric dose

Dose: Not established N/A/kg
Route: N/A
Frequency: N/A
Max: N/A
Not licensed in paediatrics

Dose adjustments

Renal

No dose adjustment required for CrCl ≥15 mL/min; limited data below

Hepatic

Severe hepatic impairment: reduce to 80 mg twice daily; monitor for adverse effects

Paediatric weight-based calculator

Not licensed in paediatrics

Clinical pearls

  • ALPINE trial (NEJM 2023): zanubrutinib superior to ibrutinib in R/R CLL — improved PFS and significantly lower atrial fibrillation rate (3.9% vs 16.0%), positioning zanubrutinib as preferred BTK inhibitor
  • Designed for more complete and sustained BTK occupancy with improved selectivity — less off-target kinase inhibition (ITK, TEC, EGFR) compared to ibrutinib, explaining lower cardiac and bleeding rates
  • MHRA 2021 approved; NICE TA795 for CLL; can be used in patients who have experienced ibrutinib-related cardiac toxicity
  • Acalabrutinib vs zanubrutinib: both are second-generation; zanubrutinib has once-daily dosing option and broader NICE approvals in CLL
  • No dose modification needed with moderate CYP3A4 inhibitors; flexible dosing (twice daily or once daily 320 mg) aids adherence

Contraindications

  • Concurrent strong CYP3A4 inhibitors without dose adjustment
  • Known hypersensitivity

Side effects

  • Neutropenia
  • Thrombocytopenia
  • Upper respiratory tract infections
  • Bruising/petechiae
  • Atrial fibrillation (lower incidence than ibrutinib)
  • Hypertension
  • Diarrhoea

Interactions

  • Strong CYP3A4 inhibitors — increase zanubrutinib exposure significantly; reduce dose to 80 mg twice daily
  • Strong CYP3A4 inducers — avoid combination; markedly reduces exposure
  • Anticoagulants/antiplatelets — additive bleeding risk

Monitoring

  • FBC (monthly first year, then periodic)
  • LFTs
  • Blood pressure
  • Cardiac monitoring (ECG if AF history)
  • Infection surveillance

Reference: BNFc; BNF 90; ALPINE trial (Brown et al. NEJM 2023); NICE TA795; MHRA SPC Brukinsa; SEQUOIA trial (Tam et al. NEJM 2022). Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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