How it is administered

Ibrutinib is taken by mouth and is available in several forms:

• Immediate-release oral capsules (70 mg and 140 mg)
• Immediate-release oral tablets (140 mg, 280 mg, and 420 mg)
• Oral suspension (70 mg/mL)

You should take ibrutinib once daily, at about the same time each day, with a glass of water. Swallow the capsules or tablets whole—do not open, break, chew, cut, crush, or chew them. For the oral suspension, follow the instructions for use provided by your healthcare team.

How it works

Ibrutinib is a small-molecule inhibitor of Bruton’s tyrosine kinase (BTK), a protein that plays a key role in the survival and spread of certain types of B-cell cancers. By forming a covalent bond with the BTK active site, ibrutinib blocks its activity. This disrupts important signaling pathways that cancerous B-cells use to grow, move, and stick to other cells.

By inhibiting BTK, ibrutinib can slow down or stop the growth of malignant B-cells, making it effective in treating certain blood cancers. In clinical studies, ibrutinib has shown the ability to reduce cancer cell proliferation and survival, as well as interfere with their movement and ability to attach to other tissues. This mechanism is especially important in diseases where B-cells are the source of the cancer, such as some lymphomas and leukemias.

Who Should take it

Ibrutinib is approved for adults with certain B-cell blood cancers, including:

• Chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL)
• CLL/SLL with 17p deletion
• Waldenström’s macroglobulinemia (WM)
• Chronic graft-versus-host disease (cGVHD) after failure of other systemic therapies (in adults and children age 1 year and older)

While ibrutinib is not specifically approved for Marginal Zone Lymphoma (MZL) in the FDA label provided, it is commonly used in other B-cell malignancies. If you have a B-cell blood cancer, your doctor may consider ibrutinib as part of your treatment plan based on your specific diagnosis and previous treatments.

Who should not take it

There are no absolute contraindications listed for ibrutinib in the FDA label. However, certain patients should use caution or may not be suitable for this medication:

• Patients with a known hypersensitivity to ibrutinib or any of its components
• Patients with severe hepatic (liver) impairment should avoid ibrutinib
• Pregnant women should not take ibrutinib, as it can cause fetal harm
• Women should not breastfeed during treatment and for at least 1 week after the last dose

Patients with a history of significant bleeding, infections, heart rhythm problems, or uncontrolled high blood pressure should discuss risks and benefits with their doctor before starting ibrutinib.

Commonly used with

Ibrutinib can be used alone or in combination with other medications, depending on the type of blood cancer being treated. Common combinations include:

• Rituximab (for CLL/SLL and WM)
• Obinutuzumab (for CLL/SLL)
• Bendamustine and rituximab (for CLL/SLL)

Your doctor will decide the best combination for your specific situation.

Commonly tested with

Ibrutinib has been tested in combination with several other medications in clinical trials, including:

• Rituximab
• Obinutuzumab
• Bendamustine
• Chlorambucil
• Fludarabine
• Cyclophosphamide

These combinations are used to determine the most effective regimen for treating different types of B-cell blood cancers.