Regorafenib (Stivarga®)

Last Modified: January 11, 2013

Pronounced: re" goe raf' e nib
Classification: Tyrosine Kinase Inhibitor

Facts about regorafenib

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 that 30% fat). 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 include:

  • 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, dexamethasone, 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.


Keep regorafenib in the container it comes in, at room temperature, and not in a pill box. The bottle contains a desiccant that keeps the medication dry, which you should not remove. Keep the bottle tightly closed.

Side effects of regorafenib

Below are some of the possible side effects and suggestions for dealing with them. Be sure to tell your oncology team if you are experiencing any of these problems.

High Blood Pressure

High blood pressure (hypertension) was seen in clinical trials and typically occurred within the first cycle of therapy. Patients should have their blood pressure checked once a week for the first 6 weeks and then regularly during therapy. Any hypertension should be treated appropriately. If hypertension cannot be controlled, the regorafenib dose 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 and 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. Read Low Fiber Diet for Diarrhea for more tips.

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.

Read the mouth ulcer tip sheet for more information.


While on cancer treatment 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 and see OncoLink’s section on fatigue for helpful tips on dealing with this side effect.

Decrease in Appetite

Visit OncoLink's section on Nutrition for tips on dealing with this side effect. Ask your nurse about nutritional counseling services.

  • 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 dislike foods or beverages that you liked before receiving chemotherapy. These symptoms can last up to several months.
  • 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.
  • Flavor meat or fish by marinating it in sweet juices, sweet and sour sauce or dressings. Use seasonings like basil, oregano or rosemary. Bacon, ham and onion can also add flavor to vegetables.

Hand and Foot Syndrome (HFS)

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. It can start as a feeling of tingling or numbness in the palms and/or soles and progress to swelling, redness, peeling skin, and tenderness or pain. Notify your healthcare team right away if you notice any of these signs of HFS so they can make recommendations or dose changes to prevent it from getting worse. Learn more about HFS on OncoLink.

Thyroid Problems

In studies, hypothyroidism (under active thyroid) and hyperthyroidism (over active thyroid) were seen in patients taking this medication. Your doctor may perform blood tests to check the function of your thyroid and treat this side effect if it develops. Symptoms of thyroid problems include: tiredness, feeling hot or cold, change in your voice, weight gain or loss, hair loss and muscle cramps.

Reproductive Concerns

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. Even if your menstrual cycle stops or you believe your sperm is affected, effective birth control is necessary during treatment and up to 2 months after stopping therapy.

Other Rare, But Emergent Side Effects

Regorafenib can cause liver toxicity, which your doctor may monitor for using blood tests called liver function tests. Notify your doctor if you develop any yellowing of the eyes or skin or dark, tea-colored urine, as this can be a sign of liver dysfunction.

Studies did not evaluate wound healing with regorafenib, but other medications in the same category do affect wound healing. Therefore, the manufacturer recommends stopping the drug at least 2 weeks before any surgical procedure and considering not restarting until there is adequate wound healing.

A neurologic complication, called reversible posterior leukoencephalopathy syndrome, has been reported. If you experience headache, seizure, confusion, blindness or other visual changes, inform your healthcare provider right away.

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.

Some patients experienced bleeding or a tear in the intestinal wall. Signs of these problems include: unexpected bleeding, blood in the stool or black stools, cough up or vomit blood or vomit that looks like coffee grounds, fever, severe pain in the abdomen or new abdominal swelling. If you experience any of these, contact your healthcare provider immediately or go to the emergency room.


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