[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [BTK inhibitors](https://durgical.com/en/pharmacology/classes/btk-inhibitors/) › Zanubrutinib

# Zanubrutinib

## BTK inhibitors?

BTK inhibitors

## High alert?

An error with this medicine can cause serious harm: double checks and protocols are used.

## Pregnancy: avoid?

Avoid in pregnancy. Zanubrutinib can harm the fetus: a pregnancy test is done first, women and men use contraception during treatment and for a week after, and breastfeeding is…

A second-generation covalent BTK inhibitor for CLL and several B-cell lymphomas. Watch for bleeding, infections and heart rhythm problems.

Updated Nov 12, 2026

## Quick facts

**Group**
[BTK inhibitors](https://durgical.com/en/pharmacology/classes/btk-inhibitors/)

**Target**
Bruton tyrosine kinase (BTK)

**Used for**
Chronic lymphocytic leukaemia

**Key effects**
Diarrhoea · Rash · Muscle

**Monitor**
Complete blood count · Signs of bleeding and infection

**ATC**
L01EL03

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**Bruton tyrosine kinase (BTK)**Zanubrutinib

ⓘ The crystal shows zanubrutinib in the ATP site of the human BTK kinase domain.

**Target in 3D:** Bruton tyrosine kinase (BTK). PDB structure 6J6M (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6J6M) · Drag to rotate · pinch to zoom

B-cell receptor signalling runs through Bruton tyrosine kinase (BTK). Zanubrutinib binds covalently to cysteine 481 in the ATP site of BTK and switches it off permanently. Malignant B cells lose their survival signals and die. It was designed to block BTK more selectively than ibrutinib.

- Bonds covalently to cysteine 481 of BTK
- B-cell receptor signalling stops
- Malignant B cells lose survival signals and die

## Indications

- Chronic lymphocytic leukaemia or small lymphocytic lymphoma. [Chronic lymphocytic leukaemia →](https://durgical.com/en/conditions/chronic-lymphocytic-leukaemia/)
- Mantle cell lymphoma after one prior therapy, marginal zone lymphoma after anti-CD20 therapy, and follicular lymphoma with obinutuzumab after two prior therapies. [Non-Hodgkin lymphoma →](https://durgical.com/en/conditions/non-hodgkin-lymphoma/)
- Waldenström macroglobulinaemia. [MGUS and Waldenström macroglobulinaemia →](https://durgical.com/en/conditions/mgus-and-waldenstrom-macroglobulinaemia/)

## Adverse effects

### Common

- Diarrhoea, constipation, nausea
- Rash, bruising
- Muscle, joint and back pain, muscle spasms
- Fatigue, headache, limb swelling
- Upper respiratory infections

### Serious (rare, important)

- Bleeding, including inside the head and gut
- Serious infections and hepatitis B reactivation
- Atrial fibrillation and other arrhythmias
- Neutropenia, thrombocytopenia, anaemia
- Second primary cancers, especially skin cancer

## Contraindications

- Hypersensitivity to zanubrutinib

## Key interactions

**St John's wort**
Can lower zanubrutinib levels; avoided.

**Omeprazole and other medicines**
Listed as interacting; the medication list is reviewed.

**Grapefruit and its juice**
Can raise zanubrutinib levels; discussed with the treating team.

## What is monitored

- Complete blood count
- Signs of bleeding and infection; hepatitis B status before starting
- Pulse and heart rhythm; blood pressure
- Skin checks and liver tests

## Administration and safety

- Oral capsules swallowed whole with water, not opened, chewed or crushed.
- It is usually held for a period before and after surgery or dental procedures because of bleeding risk.

## Pregnancy and breastfeeding

Avoid in pregnancy. Zanubrutinib can harm the fetus: a pregnancy test is done first, women and men use contraception during treatment and for a week after, and breastfeeding is stopped.

## Nursing care

- Teach to report bleeding, black stools, severe headache or confusion.
- Teach to report palpitations, dizziness or fainting.
- Sun protection and skin self-checks.
- Tell surgeons and dentists about the drug; contraception during treatment and shortly after.

## Pharmacokinetics

**Absorption**
Oral capsules or tablets once or twice a day, with or without food.

## Memory aid

«-brutinib binds Bruton»: ibrutinib, acalabrutinib and zanubrutinib all lock cysteine 481 of BTK; zanubrutinib is the more selective sibling.

## Test yourself

Think of the answer, then tap the question to see it.

## Which residue of BTK does zanubrutinib bond covalently?

Cysteine 481.

## Which three serious class adverse effects do covalent BTK inhibitors share?

Bleeding, infections and atrial fibrillation (also cytopenias and second cancers).

## Which B-cell cancers is zanubrutinib used for?

CLL/SLL, mantle cell, marginal zone and follicular lymphoma, and Waldenström macroglobulinaemia.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/zanubrutinib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

**Pregnancy: avoid**
Avoid in pregnancy. Zanubrutinib can harm the fetus: a pregnancy test is done first, women and men use contraception during treatment and for a week after, and breastfeeding is…

## Connections

## Related drugs 2

- [Ibrutinib](https://durgical.com/en/pharmacology/ibrutinib/)
- [Acalabrutinib](https://durgical.com/en/pharmacology/acalabrutinib/)

## Related conditions 3

- [Chronic lymphocytic leukaemia](https://durgical.com/en/conditions/chronic-lymphocytic-leukaemia/)
- [Non-Hodgkin lymphoma](https://durgical.com/en/conditions/non-hodgkin-lymphoma/)
- [MGUS and Waldenström macroglobulinaemia](https://durgical.com/en/conditions/mgus-and-waldenstrom-macroglobulinaemia/)

[← Back to the class: BTK inhibitors](https://durgical.com/en/pharmacology/classes/btk-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Zanubrutinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a620009.html) (MedlinePlus (U.S. National Library of Medicine), 2024); [RCSB PDB - 6J6M: Co-crystal structure of BTK kinase domain with Zanubrutinib](https://www.rcsb.org/structure/6J6M) (RCSB Protein Data Bank, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/medicines/895) (World Health Organization, 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EL03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/zanubrutinib/