Bosulif
BOSULIF
Bosutinib
Select product strength & quantity:
Select product strength & quantity:

Bosulif (Bosutinib)

What is Bosulif (Bosutinib)?

Bosulif (bosutinib) is a protein tyrosine kinase inhibitor medication used for the treatment of the blood cancer known as Philadelphia chromosome-positive chronic myelogenous leukemia, or Ph+ CML. This medication is typically used in those who have just been newly diagnosed with this condition or those who have not benefited from other types of therapy before trying Bosulif.

How is Bosulif Used?

Bosulif is available in tablet form and should be taken once per day with food, every day. Bosulif tablets should be swallowed whole and not chewed, split, or crushed for any reason.

It is either used as the first line of treatment for Ph+ CML or used as an alternative treatment for the same condition when other types of therapies have failed to be effective for the patient.

Storage

This medication should be stored at room temperature, in the range of 68°F (20°C) and 77°F (25°C). If a patient is traveling or the medication otherwise needs to be transported for any reason, it may be exposed to temperatures no lower than 59°F (15°C) and 86°F (30°C).

Keep this medication out of the reach of children at all times.

This medication should not be handled or touched if it becomes broken or crushed.

As an anticancer medication, there are special circumstances regarding the disposal of Bosulif. Due to the risks associated with this type of medication, it is strongly recommended that patients simply return any unused Bosulif to their doctor or their doctor’s practice for safe disposal. Bosulif should never be flushed or thrown away in household trash.

Uses

Bosulif is prescribed for the treatment of Philadelphia chromosome-positive chronic myelogenous leukemia, also referred to as Ph+ CML.

How Does Bosulif Work?

This medication is a tyrosine kinase inhibitor (TKI). The enzyme known as BCR-ABL kinase encourages the development and worsening of CML, and Bosulif functions by inhibiting this enzyme. It is capable of inhibiting 16 of the 18 current forms that exist of BCR-ABL kinase, making it incredibly effective at treating this component of CML.

Dosage

Bosulif is available as a tablet that is taken orally once per day, every day, with food. It comes in the following strengths:

  • 100 mg
  • 400 mg
  • 500 mg

The dosage that a patient will be required to take for treatment depends on their current medical status. Based on their current overall health, their age, whether they are new to using this type of medication or have previously tried other types of treatment before beginning Bosulif, any other medications they may be taking, and the severity of their current condition for which Bosulif has been described, their doctor will advise them on the appropriate dosage and may adjust the dosage later on as needed.

Patients should take the medication exactly as prescribed by their doctor. Commonly, most patients begin taking a lower dosage of Bosulif to begin with and often have that dosage increased over time.

Individuals with a new diagnosis of Ph+ CML that have not received any prior forms of treatment for the condition are generally started on a daily dose of 400 mg.

Those who have previously received other forms of treatment for Ph+ CML that proved to be ineffective or have problematic side effects are most commonly prescribed the 500 mg strength of this medication to be taken once per day.

For those who have blood, kidney, or liver disorders, these conditions may also require adjustment of the dosage by the patient’s prescribing physician. Changes to dosage may also be made if an individual has significant side effects or if treatment with the current strength of the medication becomes ineffective.

The maximum dosage of Bosulif a patient may take per day is 600 mg.

Overdose

Individuals who have overdosed on this medication have reported no serious adverse reactions from consuming excessive amounts of this medication. If you have taken too much Bosulif, you should contact your doctor or local Poison Control Center for further advice. Treatment for an overdose of this medication typically includes supportive treatment to manage the increased likelihood of side effects already associated with the medication as well as an observation period to ensure there are no significant adverse effects of a high dosage of Bosulif within one’s system.

Side Effects

Bosulif is associated with a range of different side effects. Please consult with your physician if you experience any of the following symptoms.

The most common side effects of taking Bosulif are as follows:

  • heart problems
  • stomach problems
  • fluid retention
  • liver problems
  • low blood cell counts
  • kidney problems

For individuals with newly diagnosed chronic myelogenous leukemia that begin using Bosulif for treatment, the following side effects are most commonly experienced in this particular group of patients using the medication:

  • abdominal pain
  • diarrhea
  • nausea
  • skin rash
  • liver function test changes
  • reduction of platelet counts

Patients who have begun using Bosulif for treatment of CML but have done so due to the need for a change in their treatment because prior medications and therapies were ineffective or not well-tolerated may experience a different set of side effects when using this medication. The following side effects are the ones most commonly reported for this group:

  • abdominal pain
  • coughing
  • diarrhea
  • fatigue
  • fever
  • headaches
  • liver function test changes
  • low red blood cell counts
  • low platelet counts
  • nausea
  • skin rash
  • swelling
  • vomiting

Please contact your doctor immediately if you experience any of the following additional side effects:

  • abnormal heart rhythms
  • back pain
  • chest pain
  • dizziness or lightheadedness
  • fainting
  • headache
  • increased blood pressure
  • itching
  • joint pain
  • loss of appetite
  • respiratory tract infections
  • seizures

Additionally, there are other side effects this medication may cause as well. If you experience any of the following and have difficulty managing the symptoms, please contact your physician:

  • acne
  • altered sense of taste
  • decreased appetite
  • flu-like symptoms
  • low phosphorus
  • high potassium
  • runny nose
  • sore throat

Bosulif has also been reported to cause problems with fertility in both male and female patients using the medication. Patients wishing to conceive a child in the future should discuss this risk with their doctor.

If you experience any of the above side effects or any that have not been listed and have concerns, please consult your prescribing physician for additional information and other potential treatment options if using the medication becomes intolerable.

Warnings & Precautions

Bosulif has been shown to have significant risks related to patients’ blood cells, hearts, livers, and kidneys. The following concerns are the most prominent risks associated with this medication, and all patients taking this medication for treatment should be monitored closely during the time frame that they use Bosulif.

Abnormal Heart Rhythms

Bosulif is known to cause abnormal heart rhythms to develop in some patients. A particular condition, QT prolongation, is most likely to occur in those patients who take Bosulif alongside certain medications, among these being chlorpromazine, arsenic trioxide, pentamidine, pimozide, mefloquine, moxifloxacin, quinidine, tacrolimus, thioridazine, or sotalol. These medications should not be mixed with Bosulif. Additionally, certain patients may also be at an increased risk of complications associated with abnormal heart rhythms if they have diabetes, already have a slow heart rate, have had a stroke, have nutritional deficiencies, have a family history of cardiac events, are female, or have a history of heart disease.

Children

The safety and efficacy of Bosulif have not been determined for those below the age of 18 years old.

Bone Problems

Bosulif places some patients at an increased risk of experiencing bone-related issues due to the decrease in both bone strength as well as density. This may result in patients taking Bosulif easily acquiring bone fractures. For individuals who already have difficulties with low bone density due to hormonal or nutritional causes, or those that have osteoporosis, the risk is greatly increased when taking this medication. If you are at an increased risk of bone-related health conditions or injuries, please discuss this with your prescribing physician before beginning treatment with Bosulif.

Food Interactions

Bosulif is known to interact with pomegranate, star fruit, and grapefruit juice. Patients taking Bosulif are advised to avoid these three juices and fruits when using this medication because they affect how the medication is expelled from the body, and this may lead to an excess amount of the medication present within the patient’s body and trigger significant adverse effects.

Heart Problems

Individuals taking Bosulif are at an increased risk of experiencing heart problems when using this medication. The greatest concern among the reported cardiac issues associated with this medication has been heart failure. Patients experiencing weight gain, shortness of breath, or significant swelling in their limbs (feet, hands, or ankles) should seek emergency medical assistance right away.

Hepatitis B

Patients with long-term, chronic hepatitis B that use Bosulif for treatment are likely to experience a flare-up of their symptoms. If you have been diagnosed with hepatitis B, please discuss your medical history with your prescribing physician before beginning treatment with Bosulif. In serious cases, the changes caused by Bosulif use alongside this condition have resulted in the need for a liver transplant, the patient developing liver failure, and even fatal results.

Liver Problems

Liver problems may occur when a patient uses Bosulif for the treatment of CML. Individuals taking this medication should have their liver function monitored during treatment. Those who develop dark-colored urine or have their skin or the whites of their eyes turn yellow (a condition known as “jaundice”) should contact their doctor as soon as these symptoms arise.

Pancreatitis

Using Bosulif has been linked to the development of inflammation in the pancreas. Patients with a medical history that includes pancreatitis or any similar conditions affecting the pancreas should discuss this with their doctor before beginning treatment with Bosulif. Individuals who are most at risk for pancreatitis while using Bosulif include those who have a history of alcoholism, gallstones, high triglycerides, or previous issues with pancreatitis.

Kidney Problems

Bosulif may result in some patients experiencing issues with their kidneys. When using Bosulif for treatment, patients should be monitored and have their kidney function checked regularly. Patients who experience changes in their frequency of urination or their quantity of urine when using the restroom should contact their doctor immediately, as these changes may be indicative of impairment of the kidneys.

Stomach Problems

Patients experiencing abdominal or digestive symptoms are advised to report these side effects to their prescribing physician as soon as possible. Some of the abdominal and digestive symptoms experienced by those taking Bosulif include abdominal pain, diarrhea, blood in the stools, nausea, and vomiting.

Low Blood Cell Counts

This medication is known to cause changes in a patient’s platelet levels when used for treatment. Patients taking Bosulif may develop neutropenia (low white blood cell counts), anemia (low red blood cell counts), or thrombocytopenia (low platelet counts). Individuals taking Bosulif should have blood tests performed regularly and have their blood cell counts monitored by their doctor. Any patients taking this medication that develop symptoms of an infection, a fever, blood in their stools or urine, significant bruising, or unusual bleeding should report these symptoms to their doctor immediately.

The symptoms of anemia include pale skin, shortness of breath, unusual weakness or fatigue, and dizziness.

Symptoms of blood-related changes that should be reported to the patient’s prescribing physician include blood in their urine, bleeding gums, coughing up blood, having a bloody nose, or noticing that any cuts they get do not stop bleeding.

Fluid Retention

Bosulif has been associated with excess fluid retention. Some of this fluid retention may occur in the stomach cavity, in the sacs around patients’ hearts, or even in the lining of their lungs. Patients that notice swelling in their feet, ankles, or hands; swelling that occurs all over their bodies; weight gain; shortness of breath; chest pain; or coughing should be sure to seek emergency medical attention immediately.

Symptoms of inflammation and fluid buildup around the heart include fatigue, diarrhea, feeling faint, fever, muscle aches, vomiting, shortness of breath, a pounding or rapid heartbeat, chest pain, weakness, a cough, and an irregular heartbeat.

Symptoms of a buildup of fluid around the lungs include rapid breathing, hiccups, a cough, and chest pain.

Pregnancy

Bosulif is not safe to use during pregnancy, and patients that are capable of becoming pregnant are strongly encouraged to incorporate some type of effective birth control while taking this medication. This should be done both while the patient is actively using Bosulif as well as for a minimum of four weeks after the use of this medication has ceased. Patients should contact their physician immediately if pregnancy occurs while the pregnant individual has been actively using Bosulif for treatment.

Additional Medical Conditions

If you have any of the following medical conditions, exercise caution when taking Bosulif and discuss your medical history with your doctor before beginning this medication:

  • if you are allergic to Bosulif
  • if you are allergic to any of the other ingredients in Bosulif
  • irregular heartbeat
  • low magnesium
  • low potassium
  • reduced liver function

Drug Interactions

Speak to your doctor about any medications or herbal supplements you are currently taking before beginning treatment with Bosulif. Discuss any concerns you may have with your doctor or a trusted pharmacist.

Drugs That Are Known to Interact with Bosulif

The following medications are known to interact with Bosulif and should be discussed with your prescribing physician before using them alongside treatment with Bosulif:

  • aluminum hydroxide
  • amiodarone
  • antacids
  • antiarrhythmic medications
  • antipsychotics
  • apalutamide
  • aprepitant
  • atazanavir
  • “-azole” antifungal medications
  • BCG
  • bosentan
  • calcium carbonate
  • carbamazepine
  • chloroquine
  • chlorpromazine
  • ciprofloxacin
  • cladribine cobicistatat
  • clarithromycin
  • clobazam
  • clomipramine
  • clozapine
  • conivaptan
  • corticosteroids
  • crizotinib
  • darunavir
  • dasatinib
  • dabrafenib
  • desipraminene
  • dexamethasone
  • diltiazem
  • disopyramide
  • diuretic medications (water pills)
  • domperidone
  • dronedarone
  • efavirenz
  • enzalutamide
  • erythromycin
  • etravirine
  • famotidine
  • flecainide
  • formoterol
  • furosemide
  • H2 antagonists
  • haloperidol
  • HIV non-nucleoside reverse transcriptase inhibitors
  • HIV protease inhibitors
  • hydrochlorothiazide
  • hydrocortisone
  • idelalisib
  • imatinib
  • imipramine
  • itraconazole
  • ivacaftor
  • ketoconazole
  • lansoprazole
  • laxatives
  • letermovir
  • levetiracetam
  • lopinavir
  • lumacaftor
  • macrolide antibiotics
  • magnesium hydroxide
  • mesalamine
  • methadone
  • mifepristone
  • modafinil
  • nevirapine
  • nizatidine
  • NNRTIs
  • Norfloxacin
  • ofloxacin
  • olanzapine
  • olsalazine
  • omeprazole
  • phenobarbital
  • phenytoin
  • prednisone
  • primidone
  • procainamide
  • protein kinase inhibitors
  • proton pump inhibitors
  • quetiapine
  • quinidine
  • quinine
  • quinolone antibiotics
  • rifabutin
  • rifampin
  • risperidone
  • ritonavir
  • romidepsin
  • salmeterol
  • seizure medications
  • sotalol
  • sulfasalazinetocilizumab
  • tricyclic antidepressant medications
  • topiramate
  • triamterene
  • valproic acid
  • verapamil
  • voriconazole
  • zonisamide

Other Substances That May Interact with Bosulif

The following substances are also indicated to cause interactions when used while taking Bosulif:

  • grapefruit juice
  • pomegranate
  • star fruit
  • John’s wort

Alternative Medications

For patients who are unable to take Bosulif or experiencing significant adverse side effects, alternative medications may be used to treat some of the associated conditions for which this medication is commonly prescribed:

  • asciminib (Scemblix)
  • dasatinib (Sprycel)
  • imatinib (Gleevec)
  • nilotinib (Tasigna)
  • ponatinib (Iclusig)

Frequently Asked Questions

Yes. This medication is generally used in long-term treatment for the condition for which it was prescribed. Patients that find the medication to be well-tolerated and effective will typically remain on it indefinitely.

If a patient has forgotten to take a dose of Bosulif, they should take that dose as soon as they remember. However, if more than 12 hours have passed since their regular dosing time, they should simply take the next upcoming dose and disregard the missed dose. Two doses of this medication should not be taken at the same time to “catch up” as this greatly increases the risk of adverse side effects occurring.

This medication should never be crushed, chewed, or split for any reason. Bosulif is intended to be taken as a tablet, whole and undamaged.

Of the patients who used Bosulif for treatment during a study, between 47.2% and 77.2% of these individuals were found to have no cancer symptoms and no cancerous cells detected via bloodwork by the 12-month mark of treatment.

Bosulif is a highly effective treatment for Ph+ CML, but it does not guarantee that a patient will be cured of the condition. Generally, most individuals with this diagnosis will simply have the condition well controlled for the long term, but there have been instances in which CML has been fully cured for some patients.

Yes. Bosulif is a chemotherapy medication used for the treatment of Ph+ CML.

Bosulif is produced by Pfizer Inc.

Being one of the most common side effects of this medication, an average of 70% to 85% of those taking Bosulif during a study experienced diarrhea as a side effect.

Due to Bosulif affecting a patient’s blood cells (including white blood cells), this may place patients at an increased risk of infection while using this medication for treatment. Patients using Bosulif should be extra cautious about being in crowds and practicing good hygiene to avoid sickness.

Pleural effusion, or a buildup of fluid around one’s lungs, was reported in 1% to 10% of patients using Bosulif for treatment. Patients experiencing symptoms of a fluid buildup around the lungs should seek emergency medical assistance immediately.

For those who take Bosulif to treat their CML, stopping this medication will result in worsening of their symptoms and a progression of the disease. Allowing CML to worsen will result in more serious symptoms as well as a reduction in the patient’s life expectancy.

Bosulif should be taken with food to be properly absorbed. Patients should not consume star fruit, pomegranate, grapefruit, or grapefruit juice while taking this medication due to the increased risk of side effects from these foods and juices, resulting in higher levels of the medication remaining in the patient’s system.

For patients who regularly take antacids or PPIs, Bosulif should be taken either two hours before or after taking the medications to reduce stomach acid.

The main and active ingredient in Bosulif is bosutinib monohydrate. The inactive ingredients in this medication are as follows: croscarmellose sodium, magnesium stearate, microcrystalline cellulose, poloxamer, polyethylene glycol, polyvinyl alcohol, povidone, talc, and titanium dioxide. The 100 mg and 400 mg tablets contain iron oxide yellow for coloring, and the 400 mg and 500 mg tablets contain iron oxide red for coloring.

Individuals above the age of 60 years old should be closely monitored when taking Bosulif as there is an increased risk of cardiac side effects.

Individuals with certain health conditions may be unable to Bosulif or may require additional monitoring during the use of this medication due to increased health risks. Among these high-risk conditions is anemia, those who have abnormal liver function tests, chronic heart failure, fluid in or around the heart, low levels of neutrophils, decreased blood platelets, liver problems, high levels of bilirubin, hepatitis B infection, liver impairment, fluid retention issues in the limbs, frequent diarrhea, or chronic kidney disease in stages 3A, 3B, or 4. Pregnant or breastfeeding individuals are strongly advised to avoid this medication if possible.

Pregnant and breastfeeding patients should not take Bosulif. However, those who need to breastfeed should wait at least two weeks after their last dose of this medication before doing so.