What to Know About Imbruvica (Ibrutinib)

Prevents the Growth and Spread of Certain Cancers

In This Article

Imbruvica (Ibtrutinib) is a medication that prevents the spread of certain cancers, including marginal zone lymphoma (MZL), chronic lymphocytic leukemia (CLL), and mantle cell lymphoma (MCL). It’s also prescribed for a complication following stem-cell transplant called chronic graft versus host disease, in which the body’s immune system mistakenly attacks donated cells.

Part of a class of drugs called kinase inhibitors, Imbruvica works by suppressing immune function by disrupting cellular signaling. This drug, generically known as Ibtrutinib, is taken as a pill.

White pills spilling out of prescription bottle onto orange surface - stock photo
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Uses

Primarily, Imbruvica is indicated for use to take on several conditions:

  • Mantle cell lymphoma (MCL): MCL is a rare-form of non-Hodgkin lymphoma and is a cancer that impacts the blood’s B-cells, which are part of the immune system. Imbruvica is only indicated after another initial treatment has been attempted.
  • Chronic lymphocytic leukemia (CLL): Another blood cancer that arises due to mutations of B-cells, CLL arises gradually and tends to impact older patients.
  • Chronic lymphocytic leukemia with 17p deletion: This is a rare genetic disorder that occurs due to untreated CLL. It’s seen in 5% to 9% of those diagnosed with CLL. Imbruvica may be prescribed for adults with this condition.
  • Waldenström's macroglobulinemia (WM): This is another form of non-Hodgkin lymphoma that attacks bone marrow and can severely hinder immune function. 
  • Marginal zone lymphoma (MZL): For patients with MZL, another form of non-Hodgkin lymphoma that attacks the blood’s B-cells, Imbruvica will be indicated if at least one prior treatment has not yielded the desired results. 
  • Chronic graft versus host disease: As noted above, this is a complication following bone marrow transplant, in which the body’s immune system starts attacking donated cells. Estimates vary, as this kind of therapy is relatively new, but this disease is seen in anywhere from 30% to 70% of cases.

Before Taking

As with any prescribed medication, it’s important to understand as much as possible about Imbruvica before taking it. Naturally, your doctor and pharmacist will be sure to provide you with important information about your prescription. As you start taking this drug, be mindful of how you’re feeling and don’t hesitate to seek help if anything seems awry.  

Precautions and Contraindications

The good news is that there are no contraindications for Imbruvica, meaning it should not react dangerously with other drugs or supplements you’re taking. That said, taking some other drugs may be influence efficacy (see below). Notably, for MCL and MZL this drug is only prescribed only after other, initial treatments have been attempted.

As with any prescribed drugs, Imbruvica may not be safe to take for certain populations, including those who are:

  • Pregnant: Taking this drug during pregnancy may potentially harm the developing fetus. This has been observed in animal studies that found high doses of Imbruvica to lead to birth defects. While exact risk has not been established in humans, if you’re expecting, you and your doctor will need to carefully weigh the pros and cons of this therapy.
  • Breastfeeding: While the presence of this drug in breast milk has not been established, it’s recommended that you not breastfeed while taking Imbruvica.
  • At risk of heart disease: Contradicted if you have conditions that increase the risk of cardiac problems, such as high blood pressure, irregular heartbeat, high cholesterol, tobacco smoking, or diabetes
  • Pediatric: The health and safety of this drug have not been established for children, and, as such, administration to this population is not recommended.
  • Liver problems: Given the liver’s essential role in cleansing and detoxifying blood, people who have severe liver problems, such as cirrhosis or liver failure should not be prescribed this drug. Further, Imbruvica may not be safe for those with milder liver problems.

Clearly, it’s essential that you provide as much information as you can about your health status to your doctor.

Other Kinase Inhibitors

Imbruvica is one of a class of drugs called kinase inhibitors; these work by hindering the production of kinase, a protein associated with cancer development and immune reaction.

As your doctor will tell you, there are quite a few other variants of this medication, which are split into different groups based on the specific mechanism of their action. Most notable are type I kinase inhibitors, which function by binding to active forms of kinase, and type II, of which Imbruvica is the first discovered compound, which functions on inactive kinase.

There are a great deal of kinase inhibitors that may be indicated for treatment. Besides Imbruvica, these include:

  • Bosulif (bosutinib)
  • Iressa, ZD1839 (gefitinib)
  • Jakafi (ruxolitinib)
  • Sprycel (Dasatinib)
  • Sutent (sunitinib)
  • Tarceva (erlotinib)
  • Tykerb (lapatinib)
  • Votrient (pazopanib)
  • Xalkori (crizotinib)
  • Zelboraf (vemurafenib)

Dosage

When it comes to dosage of Imbruvica, the ultimate authority on the matter will be your doctor. They will give you exact instructions regarding how much of this medication should be taken and when. That said, there are general guidelines for use, and these vary significantly based on the specific condition:

  • MCL: One dose of 560 milligrams (mg) should be taken orally, once a day until symptoms decrease or side-effects and toxicity are unbearable.
  • CLL and WM: For these conditions, 420 mg, once a day is indicated. Sometimes, Imbruvica is combined with other drugs, such as bendamustine, rituximab, or others to increase efficacy.
  • Chronic graft versus host disease: It’s recommended that 420 mg be taken to take on this condition until symptoms have subsided or toxicity and side-effects become too difficult. 

All listed dosages are according to the drug manufacturer and may need to be adjusted for your case. Check your prescription and talk to your doctor to make sure you are taking the right dose for you.

It’s important to note that Imbruvica comes in multiple strengths, from a 70-mg capsule marked “ibr 70” to a 560-mg oblong tablet marked “ibr” on one side and “560” on the other.

How to Take and Store

While your doctor may make some modifications based on your case, typically, Imbruvica should be taken with a glass of water at about the same time every day. If you miss a dose, don’t panic; just take one on the same day as soon as you remember, and then return to your normal schedule.

Should you miss a day, do not attempt to double up or make up for the missing dose. In addition, avoid eating grapefruit (or drinking grapefruit juice) and Seville oranges as these can interact with this drug and boost levels in the bloodstream. 

There is no specific protocol for overdosage of Imbruvica, though if you take too much, let your doctor know as they will want to monitor your health. A case has been reported where an excessive dose of 1680 mg—well over the prescribed daily amount—lead to liver problems. Constant monitoring of health while taking this drug is essential.

When it comes to storage of this drug, it’s recommended that you keep your pills at room temperature from 68 F to 77 F (20 C to 25 C). Be sure, too, that you keep these drugs in a safe place and away from children.

Side Effects

Consistent monitoring is essential for every prescription to succeed. If you’re taking this medication, be sure to let your doctor know if you’re feeling unwell. Stay safe, too: if you’re feeling severe side-effects, seek immediate medical attention.

Common

As with any pharmaceutical drug, use of Imbruvica can lead to a range of side effects. Most commonly, these include:

  • Diarrhea
  • Tiredness
  • Muscle and bone pain
  • Rash
  • Bruising
  • Mouth sores (stomatitis)
  • Muscle spasms
  • Nausea

Severe

In rarer cases, more severe side-effects crop up. These include:

Hemorrhage

Though relatively rare, severe bleeding events—occurring in up to six percent of cases—have been reported with administration of this drug. Notably, use has been tied to intracranial hemorrhage (bleeding in the brain), gastrointestinal bleeding, blood in the urine (hematuria), and post-operative hemorrhage (excessive bleeding during and after surgery).

Less severe bleeding cases occur in as many as half of those who take Imbruvica and are characterized by the presence of red welts or dots on the skin (petechiae) or easier bruising.

Infection

Use of this drug has also been tied to certain viral, fungal, or bacterial infections. In 14% to 29% of patients, some form of infection will take place.

Among these, progressive multifocal leukoencephalopathy, a viral infection that attacks the brain’s white matter, is particularly concerning. In addition, a severe, fungal lung infection called Pneumocystis jirovecii pneumonia may also arise. 

Cytopenias

Cytopenia is a term for when one or more of your blood cell types are lower than they should be. Of particular concern are reduced white blood cell types as with neutropenia, or anemia, in which the body doesn’t get enough oxygen due to a lack of healthy red blood cells.  

Atrial Fibrillation

Taking Imbruvica raises the risk of atrial fibrillation, which is an irregular and usually rapid heart rate. This is especially a risk in cases where patients have had previous heart problems, high blood pressure, or those with a history of this condition.

Hypertension

High blood pressure is also known to occur among anywhere from 6% to 17% of Imbruvica users. Other medications may need to be prescribed to help manage this.

Second Primary Malignancies

Some other diseases and cancers can occur as you’re taking this drug. These issues occur in an estimated 3% to 17% of cases, with non-melanoma skin cancer being the most common of these.

Tumor Lysis Syndrome

A rarer condition seen in those who take Imbruvica is tumor lysis syndrome, in which tumors release their cells into the bloodstream, leading to a number of symptoms, including nausea, muscle cramping, vomiting, diarrhea, and fatigue, among others.

Embryo-Fetal Toxicity

Research on animals has unearthed the potential for Imbruvica to cause harm to a developing fetus. Doctors carefully assess the relative advantages and risks of taking this drug during pregnancy and let patients know of any risks.

Warnings and Interactions

Largely, Imbruvica is able to coexist with other drugs and substances. That said, when prescribed alongside a class of drugs called CYP3A inhibitors dosages may need to be reduced. This includes a number of prescribed medications, such as:

  • Biaxin (clarithromycin)
  • Cardizem, Dilacor, Tiazac (diltiazem)
  • Erythromycin
  • Norvir (ritonavir)
  • Sporanox, Sporanox Pulsepak, and Onmel (itraconazole)
  • Verelan, Verelan PM, Calan SR, and Calan (verapamil)
  • Xolegel, Nizoral A-D, Nizoral, and Extina (ketoconazole)

In addition, some other medications, foods, herbs, and supplements have been found to influence CYP3A inhibition, which may influence the function of Imbruvica. These include:

  • Goldenseal
  • Luminal (phenobarbital)
  • Phenytek, Dilantin Infatabs, Dilantin Kapseal, Dilantin Extended, and Dilantin-125 (phenytoin)
  • Rifadin (rifampicin)
  • St. John's wort   

It’s always important to talk to your doctor about all the medications, supplements, and vitamins you’re currently taking. While some of these pose only minor interaction risks, others may be contraindicated for use. You and your doctor will need to carefully the pros and cons of treatment and any additional therapies in your case. 

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Article Sources
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  6. New Zealand Medicines and Medical Devices Safety Authority. Drug metabolism: the importance of cytochrome P450 3A4. 2014.