Ibrutinib

What is Ibrutinib?

• Ibrutinib (Imbruvica) is a kinase inhibitor used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, and Waldenstrom macroglobulinemia (a type of non-Hodgkin lymphoma).
• It is also used to treat mantle cell lymphoma and marginal zone lymphoma in patients who have received at least one other treatment.
• It is also being studied in the treatment of other types of cancer.

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What are the uses of this medicine?

This medicine is used to treat adults with:

• Mantle cell lymphoma (MCL) who have received at least one prior treatment
• Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL)
• Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion
• Waldenström’s macroglobulinemia (WM)
• Marginal zone lymphoma (MZL) who require a medicine by mouth or injection (systemic therapy) and have received a certain type of prior treatment
• Chronic graft versus host disease (cGVHD) after failure of 1 or more lines of systemic therapy

How does this medicine work?

• Ibrutinib is a small-molecule inhibitor of BTK.
• Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity.
• BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways.
• BTK’s role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion.
• Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Dose modifications of Imbruvica are recommended when used concomitantly with posaconazole, voriconazole and moderate CYP3A inhibitors.
• Avoid concomitant use of other strong CYP3A inhibitors. Interrupt Imbruvica if these inhibitors will be used short-term (such as anti-infectives for seven days or less) .
• Avoid grapefruit and Seville oranges during Imbruvica treatment, as these contain strong or moderate inhibitors of CYP3A.
• Avoid coadministration with strong CYP3A inducers (eg:(eg: rifampin, carbamazepine, phenytoin, St. John’s wort)

Is this medicine FDA approved?

• It was approved for use in the United States in 2014.

How should this medicine be used?

Recommended Dosage: Mantle Cell Lymphoma and Marginal Zone Lymphoma

• The recommended dosage of Imbruvica for MCL and MZL is 560 mg orally once daily until disease progression or unacceptable toxicity.

Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma and Waldenström’s Macroglobulinemia

• The recommended dosage of Imbruvica for CLL/SLL and WM is 420 mg orally once daily until disease progression or unacceptable toxicity.
• For CLL/SLL, Imbruvica can be administered as a single agent, in combination with rituximab or obinutuzumab, or in combination with bendamustine and rituximab (BR).
• For WM, Imbruvica can be administered as a single agent or in combination with rituximab.

Chronic Graft versus Host Disease

• The recommended dosage of Imbruvica for cGVHD is 420 mg orally once daily until cGVHD progression, recurrence of an underlying malignancy, or unacceptable toxicity.

Administration

• Take Imbruvica exactly as your healthcare provider tells you to take it.
• Take Imbruvica 1 time a day.
• Swallow Imbruvica capsules or tablets whole with a glass of water.
• Do not open, break, or chew Imbruvica capsules.
• Do not cut, crush, or chew Imbruvica tablets.
• Take Imbruvica at about the same time each day.
• If you miss a dose of Imbruvica take it as soon as you remember on the same day. Take your next dose of Imbruvica at your regular time on the next day. Do not take extra doses of Imbruvica to make up for a missed dose.
• If you take too much Imbruvica call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 70 mg and 140 mg
• Tablets: 140 mg, 280 mg, 420 mg, and 560 mg

This medicine is available in fallowing brand namesː

• Imbruvica

What side effects can this medication cause?

The most common side effects of Imbruvica in adults with B-cell malignancies (MCL, CLL/SLL, WM and MZL) include:

• diarrhea
• tiredness
• muscle and bone pain
• rash
• bruising

The most common side effects of Imbruvica in adults with cGVHD include:

• tiredness
• bruising
• diarrhea
• mouth sores (stomatitis)
• muscle spasms
• nausea
• pneumonia

Imbruvica may cause serious side effects, including:

• Bleeding problems (hemorrhage)
• Infections
• Decrease in blood cell counts
• Heart problems
• High blood pressure (hypertension)
• Second primary cancers
• Tumor lysis syndrome (TLS)

What special precautions should I follow?

• Fatal bleeding events have occurred in patients who received Imbruvica. Monitor for bleeding and manage.
• Fatal and non-fatal infections (including bacterial, viral, or fungal) have occurred with Imbruvica therapy. Monitor patients for fever and infections, evaluate promptly, and treat.
• Cytopenias may occur. Check complete blood counts monthly.
• Fatal and serious cardiac arrhythmias and cardiac failure have occurred with Imbruvica. Monitor for symptoms of arrhythmias and cardiac failure and manage.
• Hypertension occurred in 19% of 1,476 patients who received Imbruvica. Monitor blood pressure and treat.
• Other malignancies have occurred in patients, including skin cancers, and other carcinomas.
• Tumor lysis syndrome has been infrequently reported with Imbruvica. Assess baseline risk and take precautions. Monitor and treat for TLS.
• Imbruvica Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

Management of overdosage:

• Closely monitor patients who ingest more than the recommended dosage and provide appropriate supportive treatment.

Can this medicine be used in pregnancy?

• Imbruvica can cause fetal harm based on findings from animal studies.
• There are no available data on Imbruvica use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.

Can this medicine be used in children?

• The safety and effectiveness of Imbruvica in pediatric patients has not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: ibrutinib
• Inactive ingredients:
• Imbruvica capsules: croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. The 70 mg capsule shell contains gelatin, titanium dioxide, yellow iron oxide, and black ink. The 140 mg capsule shell contains gelatin, titanium dioxide, and black ink.
• Imbruvica tablets: colloidal silicon dioxide, croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, and sodium lauryl sulfate. The film coating for each tablet contains ferrosoferric oxide (140 mg, 280 mg, and 420 mg tablets), polyvinyl alcohol, polyethylene glycol, red iron oxide (280 mg and 560 mg tablets), talc, titanium dioxide, and yellow iron oxide (140 mg, 420 mg, and 560 mg tablets).

Who manufactures and distributes this medicine?

Distributed and Marketed by: Pharmacyclics LLC Sunnyvale

• Marketed by: Janssen Biotech, Inc. Horsham, PA USA

What should I know about storage and disposal of this medication?

• Store Imbruvica capsules and tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Imbruvica capsules in the original container with the lid tightly closed.
• Keep Imbruvica tablets in the original carton.
• Keep Imbruvica and all medicines out of the reach of children.

• Dailymed label info on Ibrutinib
• FDA Ibrutinib

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