Classification: Tyrosine Kinase Inhibitor
About Regorafenib (Stivarga®)
Regorafenib is a type of targeted therapy called a tyrosine kinase inhibitor. This means it works by targeting receptors present on the cancer cells. Regorafenib targets several different receptors, which, in turn, blocks tumor growth and angiogenesis (the development of a blood supply to the tumor).
How to Take Regorafenib
Regorafenib comes in a tablet form and is taken once a day, for 21 out of a 28 day cycle (3 weeks on, 1 week off). The manufacturer advises that the tablet be swallowed whole after a low-fat breakfast (containing less than 600 calories and less than 30% fat). Do not break, chew or crush the tablets. If you miss a dose, take it as soon as you remember on that day, but do not take 2 doses in one day to make up a missed dose.
Examples of a low-fat breakfast includes:
- 2 slices of white toast with 1 tablespoon of low-fat margarine and 1 tablespoon of jelly, and 8 ounces of skim milk (319 calories and 8.2 grams fat).
- 1 cup of cereal, 8 ounces of skim milk, 1 slice of toast with jelly, apple juice, and 1 cup of coffee or tea (520 calories and 2 grams fat).
The blood levels of this medication can be affected by certain foods and medications, so they should be avoided. These include: grapefruit, grapefruit juice, ketoconazole, rifampin, phenytoin, St. John’s wort, and many anti-fungal medications. Be sure to tell your healthcare provider about all medications and supplements you take.
Storage and Handling
Store your medication in the original, labeled container at room temperature and in a dry location (unless otherwise directed by your pharmacist). This medication should not be stored in a pillbox. Do not remove the desiccant packet from the container, as this keeps the environment in the bottle dry. Keep containers out of reach of children and pets. Ask your oncology team where to return any unused medication for disposal. Do not flush down the toilet or throw in the trash.
Where do I get this medication?
Regorafenib is available through select specialty pharmacies. Your oncology team will work with your prescription drug plan to identify an in-network specialty pharmacy for distribution of this medication and shipment directly to your home.
This medication may be covered under your prescription drug plan. Patient assistance may be available to qualifying individuals without prescription drug coverage. Co-pay cards, which reduce the patient co-pay responsibility for eligible commercially (non-government sponsored) insured patients, are also available. Your care team can help you find these resources, if they are available.
Possible Side Effects of Regorafenib
There are a number of things you can do to manage the side effects of regorafenib. Talk to your doctor or nurse about these recommendations. They can help you decide what will work best for you. These are some of the most common side effects:
High Blood Pressure
This medication can cause high blood pressure (hypertension). Patients should have their blood pressure checked regularly during therapy. Any hypertension should be treated appropriately. If hypertension cannot be controlled, the medication may be stopped.
Your oncology team can recommend medications to relieve diarrhea. Also, try eating low-fiber, bland foods, such as white rice and boiled or baked chicken. Avoid raw fruits, vegetables, whole grain breads, cereals and seeds. Soluble fiber is found in some foods and absorbs fluid, which can help relieve diarrhea. Foods high in soluble fiber include: applesauce, bananas (ripe), canned fruit, orange sections, boiled potatoes, white rice, products made with white flour, oatmeal, cream of rice, cream of wheat, and farina. Drink 8-10 glasses on non-alcoholic, un-caffeinated fluid a day to prevent dehydration.
Decrease in Appetite
Nutrition is an important part of your care. Cancer treatment can affect your appetite and, in some cases, the side effects of treatment can make eating difficult. Ask your nurse about nutritional counseling services at your treatment center to help with food choices.
- Try to eat five or six small meals or snacks throughout the day, instead of 3 larger meals.
- If you are not eating enough, nutritional supplements may help.
- You may experience a metallic taste or find that food has no taste at all. You may dislike foods or beverages that you liked before receiving cancer treatment. These symptoms can last for several months or longer after treatment ends.
- Avoid any food that you think smells or tastes bad. If red meat is a problem, eat chicken, turkey, eggs, dairy products and fish without a strong smell. Sometimes cold food has less of an odor.
- Add extra flavor to meat or fish by marinating it in sweet juices, sweet and sour sauce or dressings. Use seasonings like basil, oregano or rosemary to add flavor. Bacon, ham and onion can add flavor to vegetables.
Mouth Ulcers (Sores)
Certain cancer treatments can cause sores or soreness in your mouth and/or throat. Notify your doctor or nurse if your mouth, tongue, inside of your cheek or throat becomes white, ulcerated or painful. Performing regular mouth care can help prevent or manage mouth sores. If mouth sores become painful, your doctor or nurse can recommend a pain reliever.
- Brush with a soft-bristle toothbrush or cotton swab twice a day.
- Avoid mouthwashes that contain alcohol. A baking soda and/or salt warm water mouth rinse (2 level teaspoons of baking soda or 1 level teaspoon salt in an eight ounce glass of warm water) is recommended 4 times daily.
- If your mouth becomes dry, eat moist foods, drink plenty of fluids (6-8 glasses), and suck on sugarless hard candy.
- Avoid smoking and chewing tobacco, drinking alcoholic beverages and citrus juices.
This medication can cause changes to your voice including hoarseness.
Fatigue is very common during cancer treatment and is an overwhelming feeling of exhaustion that is not usually relieved by rest. While on cancer treatment, and for a period after, you may need to adjust your schedule to manage fatigue. Plan times to rest during the day and conserve energy for more important activities. Exercise can help combat fatigue; a simple daily walk with a friend can help. Talk to your healthcare team for helpful tips on dealing with this side effect.
Hand Foot Syndrome
Hand and foot syndrome (HFS) is a skin reaction that appears on the palms of the hands and/or the soles of the feet as a result of certain chemotherapy agents being absorbed by the skin cells. HFS can begin as a mild tingling, numbness, pins-and-needles feeling, or pain or swelling of the hands and/or feet. This can then progress to painful swelling, blistering or peeling skin that can interfere with your ability to do normal activities. Be sure to let your oncology team know right away if you notice these symptoms, as they may need to adjust the chemotherapy dose or take a break to allow the skin to heal. Some tips to help prevent HFS include:
- Avoid tight shoes or socks.
- Avoid activities that put pressure on the palms or soles for 1 week after treatment.
- Apply moisturizer liberally and often.
- Avoid hot water for baths and showers.
Skin, Hair & Nail Changes
Some patients may develop a rash, very dry, or itchy skin. Use an alcohol free moisturizer on your skin and lips; avoid moisturizers with perfumes or scents. Your doctor or nurse can recommend a topical medication if itching is bothersome. Your nails may become dark, brittle or fall off. If your skin does crack or bleed or you lose a nail, be sure to keep the area clean to avoid infection. While receiving this medication the hair on your head may become curly, fine or brittle. This tends to resolve once treatment is stopped.
Be sure to notify your healthcare provider of any rash that develops, as this can be a reaction and can become severe. They can give you more tips on caring for your skin, hair and nails.
Serious bleeding has also occurred in patients treated with this medication. People who have a history of serious bleeding should not take this medication. If you take aspirin, non-steroidal anti-inflammatory medications (i.e. Motrin, ibuprofen, naproxen) or other medication that interferes with blood clotting, let your healthcare provider know. Signs of bleeding can include: blood in the stool or dark, tarry stools, coughing up or vomiting blood or vomit that looks like coffee grounds. While some bleeding, such as a nosebleed, may not seem like much of a concern, you should notify your healthcare team right away if you develop bleeding of any sort.
This medication can lead to slower or incomplete wound healing, such as a surgical wound not healing or staying closed. Therefore, it is recommended that the medication be discontinued prior to any surgery. In addition, any surgical incision should be fully healed prior to starting or restarting the medication. If you have a surgical wound that has not healed or begins to have signs of infection (redness, swelling, warmth), report this to your healthcare team.
GI Tear or Fistula
This medication can cause a tear in the intestinal wall, also called a gastrointestinal perforation, or a fistula (whole connecting two parts of your GI tract). Signs of this can include: new or worsening pain in the abdomen, new abdominal swelling, chills, fever, constipation, nausea or vomiting. If you experience any of these, contact your healthcare provider immediately or go to the emergency room.
Reversible Posterior Leukoencephalopathy Syndrome (RPLS)
A neurologic complication, reversible posterior leukoencephalopathy syndrome, has been reported. If you experience headache, seizure, confusion, blindness or other visual changes, inform your healthcare provider right away.
This medication can cause liver toxicity, which your doctor may monitor for using blood tests called liver function tests. Notify your healthcare provider if you notice yellowing of the skin or eyes, your urine appears dark or brown or pain in your abdomen, as these can be signs of liver toxicity.
In studies, patients experienced heart attack and chest pain. If you experience symptoms of these problems, you should contact your healthcare provider immediately or go to an emergency room. Symptoms can include: chest pain or pressure, pain in your arm, back, neck or jaw, shortness of breath or dizziness.
Exposure of an unborn child to this medication could cause birth defects, so you should not become pregnant or father a child while on this medication. Effective birth control is necessary during treatment and for at least 2 months after treatment. Even if your menstrual cycle stops or you believe you are not producing sperm, you could still be fertile and conceive. You should consult with your healthcare team before breastfeeding while receiving this medication.