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zanubrutinib

BrukinsaBruton's tyrosine kinase (BTK) inhibitor

Brukinsa (zanubrutinib) is a Bruton's tyrosine kinase (BTK) inhibitor from BeOne Medicines for several mature B-cell cancers, including mantle cell lymphoma, Waldenstrom's macroglobulinemia, marginal zone lymphoma, chronic lymphocytic leukemia and small lymphocytic lymphoma, and follicular lymphoma in combination with obinutuzumab.

This page is based on the official US label for BRUKINSA and the EMA medicine record for Brukinsa, cross-checked with MedlinePlus and the NCI Drug Dictionary; the mechanism is explained in plain language, and analogies are used only where they stay accurate.

How it works

Explains what the medicine does in the body, not dosing, side effects, or safety.

An analogy

B-cell cancers keep growing because a molecular switch called BTK stays flicked on, passing constant grow signals from the cell surface to the nucleus. Zanubrutinib fits into the switch and locks it off, so the cancer cells stop receiving the instruction to multiply.

In simple terms

Zanubrutinib is a capsule that blocks Bruton's tyrosine kinase (BTK), an enzyme B-cell cancers need to receive growth and survival signals. By switching off this signal, zanubrutinib slows or stops the growth of malignant B cells in lymphomas and leukemias.

In depth

Zanubrutinib is a selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It covalently occupies the ATP-binding site of BTK, blocking B-cell antigen receptor (BCR) signalling and downstream survival pathways such as NF-kB and ERK. This inhibits B-cell activation, proliferation, and survival, reducing malignant B-cell growth in mantle cell lymphoma, Waldenstrom's macroglobulinemia, marginal zone lymphoma, CLL/SLL, and follicular lymphoma.

See it in motion

A schematic animation of the mechanism — simplified for clarity, not drawn to scale.

How zanubrutinib covalently occupies the ATP-binding site of BTK

Bruton's tyrosine kinase (BTK)zanubrutinibmalignant B-cell growth
  1. B-cell cancers keep growing because a molecular switch called BTK stays flicked on, passing constant grow signals from the cell surface to the nucleus.
  2. Zanubrutinib is a selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK).
  3. It covalently occupies the ATP-binding site of BTK, blocking B-cell antigen receptor (BCR) signalling and downstream survival pathways such as NF-kB and ERK.
  4. This inhibits B-cell activation, proliferation, and survival, reducing malignant B-cell growth in mantle cell lymphoma, Waldenstrom's macroglobulinemia, marginal zone lymphoma, CLL/SLL, and follicular lymphoma.
How zanubrutinib works

Target: Bruton's tyrosine kinase (BTK)

An enzyme inside B cells that relays survival and growth signals from the B-cell receptor; many B-cell cancers depend on this signal.

Approved uses

Approved uses differ by country and change over time. Always follow your local prescribing information.

Approved uses in United States

FDA
  • Mantle cell lymphoma (MCL) in adults who have received at least one prior therapy
  • Waldenstrom's macroglobulinemia (WM) in adults
  • Relapsed or refractory marginal zone lymphoma (MZL) in adults who have received at least one anti-CD20-based regimen
  • Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) in adults
  • Relapsed or refractory follicular lymphoma (FL) in adults, in combination with obinutuzumab, after two or more lines of systemic therapy

Approved uses in European Union

EMA
  • Waldenstrom's macroglobulinaemia (WM) in adults as monotherapy after at least one prior therapy, or in first-line treatment for patients unsuitable for chemo-immunotherapy
  • Marginal zone lymphoma (MZL) in adults as monotherapy after at least one prior anti-CD20-based therapy
  • Chronic lymphocytic leukemia (CLL) in adults as monotherapy
  • Refractory or relapsed follicular lymphoma (FL) in adults, in combination with obinutuzumab, after at least two prior systemic therapies

Official sources

The statements on this page trace back to these records.

  1. openFDA drug label record for zanubrutinib (Brukinsa)

    U.S. Food and Drug Administration, openFDA

  2. MedlinePlus: zanubrutinib

    MedlinePlus, U.S. National Library of Medicine

  3. NCI Drug Dictionary: zanubrutinib

    National Cancer Institute

This page explains how the medicine works — it isn’t the patient leaflet. For anything that applies to you, read the leaflet that came with your medicine or ask your pharmacist.

MedUnfold provides educational content and is not medical advice. Always follow your local prescribing information and healthcare professional.