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ibrutinib (Imbruvica)
Tyrosine Kinase Inhibitors

How it is administered

Ibrutinib is taken by mouth, available as immediate-release oral capsules, tablets, and an oral suspension. The most common dosage for Waldenström’s Macroglobulinemia is 420 mg once daily, taken at about the same time each day. Capsules and tablets should be swallowed whole with water—do not open, break, or chew them. The oral suspension comes with specific instructions for dosing and administration.

If a dose is missed, it should be taken as soon as possible on the same day, and the regular schedule resumed the next day. Do not take extra doses to make up for a missed dose.

How it works

Ibrutinib is a targeted therapy known as a Bruton’s tyrosine kinase (BTK) inhibitor. BTK is a protein that plays a key role in the signaling pathways that help certain blood cancer cells (B-cells) survive and grow. By binding to and blocking BTK, ibrutinib disrupts these pathways, which can slow down or stop the growth of cancerous B-cells.

In Waldenström’s Macroglobulinemia, a type of blood cancer involving abnormal B-cells, ibrutinib helps to reduce the number of these cells, control symptoms, and slow disease progression. Its action is specific to B-cell cancers, making it an effective option for patients with this condition.

Common side effects

  • Diarrhea
  • Bruising
  • Thrombocytopenia (low platelets)
  • Neutropenia (low white blood cells)
  • Nausea
  • Rash
  • Fatigue
  • Musculoskeletal pain (muscle/joint aches)
  • Hemorrhage (bleeding)
  • Hypertension (high blood pressure)
  • Infections (including upper respiratory tract infections and pneumonia)
  • Headache
  • Dizziness

Most side effects are manageable, but some may be serious. Always report any unusual symptoms, especially signs of bleeding, infection, or heart rhythm changes, to your healthcare provider.

Who Should take it

Ibrutinib is indicated for adults with Waldenström’s Macroglobulinemia (WM), a rare type of non-Hodgkin lymphoma. It can be used as a single agent or in combination with rituximab. It is also approved for other B-cell malignancies, such as chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL).

Patients who have been diagnosed with WM and need treatment due to symptoms or disease progression may benefit from ibrutinib. Decisions about starting ibrutinib should be made in consultation with a hematologist or oncologist familiar with your specific case.

Who should not take it

There are no absolute contraindications listed for ibrutinib, but certain patients should use it with caution or may need to avoid it. Patients with severe liver impairment should not take ibrutinib. It should also be avoided during pregnancy and breastfeeding, as it can cause harm to a developing fetus or nursing infant.

People with a history of severe bleeding disorders, recent major surgeries, or uncontrolled infections should discuss risks with their doctor. Ibrutinib may interact with other medications, especially those affecting liver enzymes (CYP3A inhibitors/inducers), so always inform your healthcare provider about all medicines and supplements you are taking.

Commonly used with

In Waldenström’s Macroglobulinemia, ibrutinib can be used alone or in combination with rituximab, another medication that targets B-cells. In other blood cancers, it may also be combined with other agents such as obinutuzumab or bendamustine and rituximab.

Your doctor will decide the best combination based on your diagnosis, previous treatments, and overall health.

Commonly tested with

Ibrutinib has been tested in clinical trials both as a single agent and in combination with rituximab for Waldenström’s Macroglobulinemia. In other blood cancers, it has been studied with combinations including obinutuzumab, bendamustine, and other chemotherapy or immunotherapy agents.

Clinical trials continue to explore new combinations and uses for ibrutinib in various blood cancers.

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