9 mins read

Overview: Regorafenib is used to treat certain cancers. Common side effects include stomach pain, diarrhea, and tiredness. Call your health care provider right away if you have yellowing of your skin or the white part of your eyes, severe nausea or vomiting, or dark pee or poop. Get emergency help if you have trouble breathing, chest pain, or an abnormal heartbeat.

Uses

What is regorafenib used for?

Regorafenib is commonly used to treat certain types of the following cancers. 

Regorafenib may also be used for other conditions as determined by your health care provider.

How does regorafenib work (mechanism of action)?

Regorafenib is a type of medicine known as a tyrosine kinase inhibitor (TKI). Kinases are proteins that have a role in cancer development, growth, and spread. By inhibiting many different kinases, regorafenib can cause cancer cells to die and prevent cancer cells from growing or spreading.

How is regorafenib supplied (dosage forms)?

Brands and other names

  • Stivarga

Dosage forms and strengths

  • 40 mg oral tablets

How should I store regorafenib?

Regorafenib should be stored at room temperature, between 68 F and 77 F (20 C and 25 C). It can be exposed to temperatures between 59 F and 86 F (15 C and 30 C) for shorter periods of time, such as when transporting it. Store in a cool, dry place. 

Keep regorafenib in the original bottle. The bottle will also have a desiccant packet to help protect the medicine from moisture. Do not remove the packet. Throw away any medicine that is not used seven weeks after opening the bottle.

Side Effects

What are the most common side effects of regorafenib?

The most common side effects of regorafenib are listed below. Tell your health care provider if you have any of these side effects that bother you.

  • Stomach pain
  • Feeling unusually weak or tired
  • Diarrhea
  • Loss of appetite
  • Infections (see below)
  • Hand-foot syndrome (see below)
  • Changes in your voice
  • Increases in liver function tests
  • Fever
  • Mouth sores
  • Weight loss

There may be other side effects of regorafenib that are not listed here. Contact your health care provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088. In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of regorafenib?

While less common, the most serious side effects of regorafenib are described below, along with what to do if they happen.

Severe Allergic Reactions. Regorafenib may cause allergic reactions, which can be serious. Stop taking regorafenib and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

Liver Damage. Liver damage, also called hepatotoxicity, can happen when taking regorafenib. Call your health care provider right away if you have any of the following symptoms of liver damage.

  • Nausea or vomiting
  • Stomach or belly pain
  • Fever
  • Weakness or unusual tiredness
  • Itching
  • Loss of appetite
  • Light-colored poop
  • Dark-colored urine (pee)
  • Your skin or the whites of your eyes turning yellowish in color (also called jaundice)

Infections. Regorafenib can increase your risk of infections, including serious infections. Call your health care provider right away if you have an infection or any of the following symptoms.

  • Burning or stinging when you pee
  • Cough or coughing up blood
  • Fever, sweats, chills, or muscle aches
  • Shortness of breath
  • Diarrhea or stomach pain
  • Severe sore throat
  • Redness, swelling, or pain anywhere in your body

Severe Bleeding. Regorafenib can increase your risk of severe bleeding that can lead to death. Some people with serious bleeding may need a blood transfusion or surgery. Call your health care provider right away if you have unusual bruising or any of the following signs of severe bleeding while taking regorafenib.

  • Pink, red, or brown urine (pee)
  • Vomit with blood that looks like coffee grounds
  • Red or black stools (looks like tar)
  • Coughing up blood or blood clots
  • Stomach pain that does not go away
  • Unusual vaginal bleeding
  • Feel faint

Stomach or Intestinal (Gastrointestinal) Tears. Regorafenib may cause a tear in your stomach or intestinal wall called a bowel perforation. This can be serious and sometimes lead to death. Tell your health care provider right away if you have any of the following signs or symptoms of bowel perforation.

  • Severe pain in your stomach area
  • Swelling of your stomach area
  • Fever or chills
  • Nausea or vomiting
  • Dehydration

Severe Skin Reactions. Regorafenib can cause severe skin reactions, called Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), that can lead to death if not treated. If you develop a rash, stop regorafenib and call your health care provider right away. Get emergency help if you have any of the following symptoms of SJS or TEN.

  • Painful red or purple skin that looks burned and peels off
  • Flat red rash or blisters on your skin, mouth, nose, and genitals
  • Red, painful, watery eyes
  • Flu-like symptoms including fever, chills, and muscle aches

Hand-Foot Syndrome. Regorafenib can cause "hand-foot" syndrome, also called palmar-plantar erythrodysesthesia syndrome. Hand-foot syndrome can cause you to have numbness, tingling, or changes in feeling in the palms of your hands and soles of your feet. It may also cause redness, swelling, or pain in your hands and feet. Stop taking regorafenib and call your health care provider right away if you have any of these symptoms and cannot do your usual activities.

Increased Blood Pressure (Hypertension). Regorafenib may increase your blood pressure or make it worse if you have a history of high blood pressure. Call your health care provider if your blood pressure increases while taking this medicine.

If you measure your blood pressure and the top number (systolic) is 180 or higher or the bottom number (diastolic) is 120 or higher, get medical attention right away. Increases in blood pressure may not be noticeable, but look out for and tell your health care provider right away if you have any of the following symptoms of severely high blood pressure.

  • Sudden severe headache
  • Chest pain
  • Dizziness or confusion
  • Trouble breathing
  • Nausea or vomiting
  • Blurry or other changes to vision
  • Anxiety
  • Buzzing in the ears
  • Nosebleed
  • Feeling of skipped heartbeats

Heart Attack. Regorafenib can increase your risk of a heart attack that can lead to death. Get emergency help if you have any of the following symptoms of a heart attack.

  • Chest pain or pressure
  • Fast or abnormal heartbeat
  • Trouble breathing
  • Pain in your back, jaw, throat, or arm
  • Sweating, upset stomach, vomiting, or dizziness

Posterior Reversible Encephalopathy Syndrome (PRES). Regorafenib may cause a rare but serious brain condition called PRES. PRES involves swelling and narrowing of blood vessels in your brain. If PRES is not treated, it can lead to a stroke. Call your health care provider right away if you have the following symptoms of PRES.

  • Changes in thinking or behavior
  • Confusion or hallucinations
  • Sudden decrease or change in vision
  • Sudden severe headache
  • Seizures

Wound Healing Issues. Regorafenib can make it difficult for your body to heal wounds. Tell your health care provider if you have any planned or emergency surgeries or if you have any injuries that occur while taking regorafenib.

Warnings & Precautions

Who should not use regorafenib?

Allergies to Ingredients. People who are allergic to any of the following should not take regorafenib.

  • Regorafenib
  • Stivarga
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in the specific regorafenib products they stock.

What should I know about regorafenib before using it?

Do not take regorafenib unless it has been prescribed to you by a health care provider. Take it as prescribed.

Do not share regorafenib with other people, even if they have the same condition as you. It may harm them.

Keep regorafenib out of the reach of children.

Your health care provider will do regular blood tests while you are taking regorafenib to make sure the medicine is safe for you. Keep all appointments with your health care provider. 

If you are of Asian descent, you may be at higher risk of certain side effects. Talk with your health care provider if this is a concern for you.

If you are able to get a partner pregnant, you should use condoms while taking regorafenib and for two months after your last dose. 

Regorafenib may make it difficult for you to get pregnant or get your partner pregnant. If you have concerns, talk to your health care provider.

What should I tell my health care provider before using regorafenib?

Tell your health care provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them determine if regorafenib is right for you.

In particular, make sure that you discuss any of the following.

Current and Past Health Conditions. Tell your health care provider if you have any of the following.

  • Heart problems, including cardiomyopathy, heart failure, heart rhythm changes, chest pain, and heart attack
  • Bleeding problems
  • High blood pressure
  • Liver problems
  • Prior or planned surgery
  • A wound that is healing
  • Skin problems
  • Stomach problems including previous ulcers or tears in your stomach

Other Medicines and Supplements. Regorafenib may interact with other medicines and supplements. Before taking regorafenib, tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

Pregnancy. Regorafenib may cause harm to a fetus. Your health care provider will give you a test to make sure you are not pregnant before you start taking regorafenib. If you can get pregnant, you should use birth control while taking regorafenib and for two months after your last dose. Tell your health care provider if you are pregnant or plan to become pregnant.

Breastfeeding. It is not known if regorafenib passes into breast milk. Do not breastfeed while taking regorafenib and for two weeks after your last dose. Tell your health care provider if you are breastfeeding or plan to breastfeed.

Interactions

Does regorafenib interact with foods or drinks?

Take regorafenib after you eat a low-fat meal. This is a meal that has less than 600 calories and less than 30% fat. Ask your health care provider if you have any questions.

Grapefruit interacts with regorafenib. Do not eat grapefruit or drink grapefruit juice while taking regorafenib. This is because grapefruit can interfere with your body’s ability to break down regorafenib, which can lead to high levels of the medicine and an increased risk of side effects. 

It is unknown if drinking alcohol will affect regorafenib, but heavy drinking can slow your immune response and make it harder for your body to fight cancer.

Does regorafenib interact with other medicines (drug interactions)?

Always tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.

In particular, make sure that you discuss if you are using any of the following before taking regorafenib.

  • St. John’s wort, which is a supplement that may be used to treat depression
  • Clarithromycin, which is a medicine used for bacterial infections
  • Itraconazole (Sporanox, Tolsura), ketoconazole, posaconazole (Noxafil), or voriconazole (Vfend), which are medicines used for fungal infections
  • Nefazodone, which is a medicine used to treat depression
  • Phenobarbital, which is a medicine that may be used to treat seizures
  • Carbamazepine (Carbatrol, Tegretol, and others), which is a medicine commonly used to treat seizures or nerve pain
  • Phenytoin (Dilantin, Phenytek, and others), which is a medicine to control seizures
  • Rifampin (Rifadin), which is a medicine commonly used to treat an infection called tuberculosis
  • Methotrexate (Trexall and others), which is a medicine commonly used for rheumatoid arthritis or certain types of cancer
  • Atorvastatin (Lipitor and others) or fluvastatin (Lescol), which are medicines to lower cholesterol

Many other medicines may alter the blood levels of regorafenib and vice versa. Tell your health care provider about all medicines that you take or have recently taken

This may not be a complete list of medicines that can interact with regorafenib. Always check with your health care provider.

Does interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much regorafenib?

If you or someone else has used too much regorafenib, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of regorafenib?

If you miss a dose, take it as soon as you remember that day. If it is the next day, skip the missed dose and only take the next dose. Do not take double or extra doses.