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How does this medication work? What will it do for me?

Ripretinib belongs to the class of medications called antineoplastic agents. Specifically, it belongs to the family of medications called protein kinase inhibitors. This medication is used to treat advanced gastrointestinal stromal tumour (GIST), a type of cancer, when other medications have been tried and either haven’t been effective or the tumour has returned.

Ripretinib is believed to prevent the growth and spread of cancer cells by blocking an enzyme that promotes cell growth.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Each white-to-off-white oval tablet debossed with "DC1" on one side of the tablet, contains 50 mg of ripretinib. Nonmedicinal ingredients: crospovidone, hypromellose acetate succinate, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and silicon dioxide.

How should I use this medication?

The recommended adult dose of ripretinib is 150 mg (three 50 mg tablets) taken by mouth, once daily. This medication may be taken with or without food, at the same time each day. Swallow the tablets whole. Do not chew, crush, or split the tablets. If a tablet is cracked, crushed, or split, do not take the tablet.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you vomit after taking a dose, do not take another dose. Continue with your regular schedule the next day.

If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is more than 8 hours after the missed dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature in its original container, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take this medication if you are allergic to ripretinib or any ingredients of the medication.

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • abdominal pain
  • back or joint pain
  • constipation
  • decreased appetite
  • diarrhea
  • dizziness
  • dry or itchy skin
  • hair thinning or loss
  • headache
  • heartburn
  • mouth sores
  • muscle spasms
  • nausea
  • swelling
  • tiredness
  • vomiting
  • weakness
  • weight loss

Although most of the side effects listed below don’t happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • fever
  • signs of hand-foot syndrome (e.g., thickening skin on palms of hands/soles of feet, tingling or burning, skin tightness)
  • signs of skin cancer (e.g., rash; new or changing skin lesions; thickening skin, rough, scaly patches; open sores; new or changing skin colour)
  • symptoms of high blood pressure (e.g., shortness of breath, dizziness or fainting, fatigue, chest pain or pressure, racing pulse or pounding heartbeat)

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
  • symptoms of decreased blood flow to the heart (e.g., chest pain, pressure or discomfort, feeling faint or anxious, shortness of breath, irregular heartbeat, nausea, sudden heavy sweating)
  • symptoms of heart failure (e.g., shortness of breath; tiredness; weakness; swelling in ankles, legs and feet; cough; fluid retention; decreased appetite; nausea; decreased ability to exercise)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Blood pressure: This medication can cause increased blood pressure. If you have high blood pressure, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Fertility: This medication can reduce male fertility. If this is a concern, talk to your doctor about methods to preserve sperm.

Heart function: Ripretinib can cause the heart to become less effective in pumping blood throughout the body. This can cause decreased blood flow to the heart muscle, heart damage, and heart attack. If you experience symptoms of heart failure, such as fluid building up in the ankles and feet, unusual tiredness, and difficulty breathing, contact your doctor as soon as possible. If you experience symptoms of heart attack, such as chest pain, shortness of breath, pressure on your chest, or pain stretching to your left shoulder, seek medical help immediately.

Kidney function: The safety and effectiveness of this medication have not been studied for people who have severely decreased kidney function. If you have kidney problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: The liver is responsible for breaking down this medication and removing it from the body. If you have decreased liver function or liver disease, ripretinib may build up in the body causing side effects.

The safety and effectiveness of this medication have not been studied for people who have moderately or severely decreased liver function. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Male contraception: This medication can cause harm to the fetus if the female partner of a man taking ripretinib becomes pregnant. Men should use effective contraception for 2 weeks before starting ripretinib, while taking ripretinib, and for at least one menstrual cycle of the female partner. This medication can also affect fertility.  Discuss any concerns you may have with your doctor before starting treatment.

Other cancers: There have been reports of squamous cell carcinoma and melanoma, two forms of skin cancer, developing after taking this medication. Skin cancer may appear as scaly red patches; open sores; or rough, thickened, or wart-like skin. It may also appear as raised growths on the skin. Report any skin changes to your doctor as soon as possible.

Sensitivity to sunlight: This medication may increase the sensitivity of the skin to sunlight or other sources of ultraviolet light, increasing the risk of sunburn. Avoid exposure to sunlight for long periods of time, particularly between the hours of 10 am and 2 pm, while you are taking this medication. Wear a broad-spectrum sunscreen and lip balm with an SPF of 30 or greater. If you notice any unusual skin rash or peeling, contact your doctor immediately.

Wound healing: This medication can cause slowed wound healing. You may find that it takes longer than normal for cuts or wounds to heal. Make sure your dentist and other members of your healthcare team are aware that you are taking this medication.

Pregnancy: This medication can cause severe birth defects if the mother takes this medication during pregnancy. Effective birth control must be used starting 2 weeks before starting ripretinib, while taking the medication and for at least one menstrual cycle after the last dose. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if ripretinib passes into breast milk. Women are advised to not breast-feed while taking this medication and for 2 weeks after taking the last dose.

Children: The safety and effectiveness of using this medication have not been established for children. 

What other drugs could interact with this medication?

There may be an interaction between ripretinib and any of the following:

  • apalutamide
  • aprepitant
  • "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • bosentan
  • clarithromycin
  • cobicistat
  • conivaptan
  • deferasirox
  • efavirenz
  • elagolix
  • enzalutamide
  • etravirine
  • fosphenytoin
  • HIV protease inhibitors (e.g., atazanavir, darunavir, indinavir, lopinavir, ritonavir)
  • lumacaftor and ivacaftor
  • mitotane
  • mifepristone
  • modafinil
  • protein kinase inhibitors (e.g., ceritinib, dabrafenib, idelalasib, palbociclib)
  • rifabutin
  • rifampin
  • St. John’s wort
  • sarilumab
  • seizure medications (e.g., carbamazepine, phenobarbital, phenytoin, primidone)
  • siltuximab
  • tocilizumab

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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Last Updated: 24/05/2024