Ibrutinib

Ibrutinib is a prescription medication used to treat patients with mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL) patients who have received at least one prior therapy. This medication is approved to treat Waldenström’s macroglobulinemia (WM), a rare form of cancer that begins in the body’s immune system. Ibrutinib is also approved to treat Marginal zone lymphoma (MZL) and chronic graft versus host disease (cGVHD). 

Ibrutinib belongs to a group of drugs called kinase inhibitors. It works by blocking the enzyme that allows cancer cells to grow and divide.

This medication comes in capsule form and is taken once a day with a full glass of water. Do not open, break, or chew the capsules.

Common side effects include diarrhea, fatigue, and muscle and joint pain.

Ibrutinib is a prescription medication used to treat patients with:

• Mantle cell lymphoma (MCL) who have received at least one prior therapy. MCL is a type of cancer that begins in the cells of the immune system.
• Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL)
• Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with a deletion in chromosome 17 (17p deletion). CLL is a rare blood and bone marrow disease that usually gets worse slowly over time, causing a gradual increase in white blood cells called B lymphocytes, or B cells.
• Waldenström’s macroglobulinemia (WM), a rare form of cancer that begins in the body’s immune system.
• 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 one or more treatments have failed.

  This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Ibrutinib may be found in some form under the following brand names:

• Imbruvica

Serious side effects have been reported with ibrutinib. See the “Ibrutinib Precautions” section.

Common side effects of ibrutinib include the following:

• diarrhea
• anemia
• fatigue
• muscle pain
• joint pain
• low platelet counts
• low white blood cell counts
• tissue swelling
• upper airway infection
• nausea
• bruising
• difficulty breathing
• constipation
• rash
• stomach pain
• vomiting
• decreased appetite

This is not a complete list of ibrutinib side effects. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with ibrutinib. See the “Ibrutinib Precautions” section.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that block a protein in the body (CYPA4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), conivaptan (Vaprisol), delavirdine (Rescriptor), and nefazodone (Serzone)
• medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), St John's wort, and nimodipine (Nimotop)

This is not a complete list of ibrutinib drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with ibrutinib including the following:

• Bleeding problems can happen during treatment with ibrutinib that can be serious. Tell your healthcare provider if you have any signs of bleeding, including: blood in your stools or black stools (looks like tar), pink or brown urine, unexpected bleeding or bleeding that is severe or that you can not control, vomit blood or vomit looks like coffee grounds, cough up blood or blood clots, increased bruising, feel dizzy or weak, confusion, change in your speech, or a headache that lasts a long time.
• Infections can happen during treatment with ibrutinib. Infections can be serious and may lead to death. Tell your healthcare provider if you have fever, chills, or any other signs or symptoms of an infection while taking ibrutinib.
• a decrease in blood cell counts. Your healthcare provider should do monthly blood tests to check your blood counts.
• High Blood pressure. Your doctor will monitor your blood pressure. New or worsening high blood pressure has happened in people treated with this medication. Your healthcare provider may start you on blood pressure medicine or change current medicines to treat your blood pressure.
• Heart rhythm problems (atrial fibrillation and atrial flutter). Heart rhythm problems have happened in people treated with ibrutinib, especially in people who have an increased risk for heart disease, have an infection, or who have had heart rhythm problems in the past. Tell your healthcare provider if you get any symptoms of heart rhythm problems, such as feeling as if your heart is beating fast and irregular, lightheadedness, dizziness, shortness of breath, chest discomfort, or you faint 
• Second primary cancers. New cancers have happened in people who have been treated with ibrutinib, including cancers of the skin or other organs.
• Tumor lysis syndrome (TLS). TLS is caused by the fast breakdown of cancer cells. TLS can cause kidney failure and the need for dialysis treatment, abnormal heart rhythm, seizure, and sometimes death. Your healthcare provider may do blood tests to check you for TLS.

This medication can cause harm to your unborn baby. Pregnancy should be avoided during treatment and for 1 month after the last dose of this medication.

Ibrutinib is not recommended in those with liver dysfunction (h moderate or severe baseline liver impairment). 

Diarrhea is a common side effect in people who take ibrutinib. Drink plenty of fluids during treatment to help lower your risk of losing too much fluid (dehydration) due to diarrhea. Tell your healthcare provider if you have diarrhea that does not go away.

Do not take ibrutinib if you are allergic to ibrutinib or to any of its ingredients.

Grapefruit and grapefruit juice may interact with ibrutinib and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before taking ibrutinib, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to ibrutinib or to any of its ingredients
• have had recent surgery or plan to have surgery. Your healthcare provider may stop Imbruvica for any planned medical, surgical, or dental procedure.
• have bleeding problems
• have liver problems
• have or had heart rhythm problems
• smoke
• have a medical condition that increases your risk of heart disease, such as high blood pressure, high cholesterol, or diabetes
• have an infection 
• are pregnant or plan to become pregnant. Ibrutinib can harm your unborn baby. You should not become pregnant while taking ibrutinib.
• are breastfeeding or plan to breastfeed. You and your healthcare provider should decide if you will take ibrutinib or breastfeed. You should not do both.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category D. It has been shown that use of ibrutinib in pregnant women caused some babies to be born with problems. However, in some serious situations, the benefit of using this medication may be greater than the risk of harm to the baby.

Pregnancy should be avoided during treatment and for 1 month after the last dose of this medication.

It is recommended men avoid getting their partners pregnant during treatment and for 1 month after the last dose of this medication. 

It is not known if ibrutinib crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using ibrutinib.

Take ibrutinib exactly as your healthcare provider tells you to take it.

• Take ibrutinib 1 time a day.
• Swallow ibrutinib capsules whole with a glass of water. Do not open, break, or chew ibrutinib capsules.
• Take ibrutinib at about the same time each day.
• If you miss a dose of ibrutinib take it as soon as you remember on the same day. Take your next dose of ibrutinib at your regular time on the next day. Do not take 2 doses of ibrutinib on the same day to make up for a missed dose.

Take ibrutinib exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The recommended dose of ibrutinib for mantle cell lymphoma (MCL) and Marginal zone lymphoma (MZL) is 560 mg (four 140 mg capsules) by mouth once daily.

The recommended dose of ibrutinib for chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma and Waldenström’s macroglobulinemia (WM), and chronic graft versus host disease is 420 mg taken orally once daily (three 140 mg capsules once daily).

For those patients with mild liver impairment, the dose of Imbruvica needs to be lowered. 

If you take too much ibrutinib, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If ibrutinib is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

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