Regorafenib is used to treat colon and rectal cancer (cancer that begins in the large intestine or the rectum) that has spread to other parts of the body. It is also used to treat gastrointestinal stromal tumors (GIST; a type of tumor that grows in the stomach, intestine [bowel], or esophagus [tube that connects the throat with the stomach]) in people who were not treated successfully with certain other medications. Regorafenib is also used to treat hepatocellular carcinoma (HCC; a type of liver cancer) in people who were previously treated with sorafenib (Nexafar). Regorafenib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps to slow or stop the spread of cancer cells.

Side Effects Of Regorafenib

Regorafenib may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • tiredness
  • weakness
  • loss of appetite
  • diarrhea
  • swelling, pain, and redness of the lining of your mouth or throat
  • weight loss
  • hoarseness or other change in the sound of your voice

Some side effects can be serious. If you experience any of these symptoms or those listed in the WARNINGS and PRECAUTIONS section, call your doctor immediately or get emergency medical treatment:

  • chest pain
  • shortness of breath
  • unusual vaginal discharge or irritation
  • burning or pain when urinating
  • dizziness or feeling faint
  • fever, cough, sore throat, chills, and other signs of infection
  • swelling of the abdomen
  • high fever
  • chills
  • severe diarrhea
  • severe headache
  • seizure
  • confusion
  • changes in vision
  • dry mouth, muscle cramps, or decreased urination
  • redness, pain, blisters, bleeding or swelling on the palms of your hands or soles of your feet
  • rash
  • vomiting blood or vomiting material that looks like coffee grounds
  • pink or brown urine
  • red or black (tarry) stools
  • coughing up blood or blood clots
  • abnormally heavy menstrual bleeding (periods)
  • unusual vaginal bleeding
  • frequent nosebleeds

Regorafenib may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

Warnings & Precautions

Before taking regorafenib:

  • tell your doctor and pharmacist if you are allergic to regorafenib, any other medications, or any of the ingredients in regorafenib tablets. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements, you are taking or plan to take. Be sure to mention any of the following: anticoagulants (”blood thinners”) such as warfarin (Coumadin, Jantoven); certain antifungal medications such as itraconazole (Onmel, Sporanox), ketoconazole (Nizoral), posaconazole (Noxafil), and voriconazole (Vfend); certain medications for seizures such as carbamazepine (Carbatrol, Epitol, Tegretol), phenobarbital, and phenytoin (Dilantin, Phenytek); atorvastatin (Lipitor, in Caduet); clarithromycin (Biaxin, in Prevpac); fluvastatin (Lescol); irinotecan (Camptosar); methotrexate (Otrexup, Rasuvo, Trexall); rifampin (Rifadin, Rifamate, in Rifater); or telithromycin (Ketek). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor what herbal products you are taking, especially St. John’s wort. You should not take St. John’s wort while taking regorafenib.
  • tell your doctor if you have a wound that has not healed or if you have or have ever had bleeding problems, high blood pressure, chest pain, or heart, kidney, or liver disease. Also, tell your doctor if you recently had surgery.
  • tell your doctor if you are pregnant or plan to become pregnant. If you are a female, you should not become pregnant while you are taking regorafenib and for up to 2 months after your final dose. Talk to your doctor about birth control methods that will work for you. If you are male, you and your female partner should use birth control during your treatment and continue to use birth control for 2 months after your final dose. If you or your partner become pregnant while taking regorafenib, call your doctor. Regorafenib may harm the fetus.
  • tell your doctor if you are breast-feeding. You should not breastfeed during your treatment with regorafenib and for up to 2 weeks after your final dose.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking regorafenib. Your doctor probably will tell you to stop taking regorafenib at least 2 weeks before your surgery. Your doctor will tell you when it is safe for you to start taking regorafenib again after your surgery.

Dosage Of Regorafenib

Regorafenib comes as a tablet to take by mouth. It is usually taken with a low-fat meal (containing under 600 calories and less than 30% of calories from fat) once a day for 3 weeks and then skipped for 1 week. This treatment period is called a cycle, and the cycle may be repeated for as long as your doctor recommends. Take regorafenib at the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take regorafenib exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the tablets whole; do not split, chew, or crush them.

Your doctor may decrease your dose of regorafenib or tell you to stop taking regorafenib for a period of time during your treatment. This will depend on how well the medication works for you and any side effects you may experience. Continue to take regorafenib even if you feel well. Do not stop taking regorafenib without talking to your doctor.

Regorafenib is not available at retail pharmacies. Your medication will be mailed to you or to your doctor from a specialty pharmacy. Ask your doctor if you have any questions about how you will receive your medication.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.


Keep all appointments with your doctor. Your doctor will check your blood pressure before you begin taking regorafenib and regularly during your treatment.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.


All information has been provided courtesy of MedLinePlus from the National Library of Medicine and from the FDA.