Regorafenib

Regorafenib is a prescription medication used to treat colon or rectal cancer that has spread (metastasized) in adults. It is also used to treat a type of tumor that occurs in the stomach or small intestine and is approved to treat a type of liver cancer called hepatocellular carcinoma (HCC). 

Regorafenib belongs to a group of drugs called kinase inhibitors, which prevent the growth and spread of cancer cells by blocking certain enzymes.

This medication comes in tablet form and is taken once a day for 3 weeks, then stopped for 1 week.  This cycle is then repeated throughout treatment. Regorafenib should be taken with a low-fat breakfast.

Common side effects include tiredness, weakness, loss of appetite, and diarrhea. 

Regorafenib is a prescription medicine used to treat people with colon or rectal cancer that has spread to other parts of the body and for which they have received previous treatment with certain chemotherapy medicines.

Regorafenib is also used to treat advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed, or has spread to other parts of the body, and no longer respond to other treatments.

This medication is also approved to treat a type of liver cancer called hepatocellular carcinoma (HCC) in adults who have been previously treated with sorafenib. 

Regorafenib may be found in some form under the following brand names:

• Stivarga

Regorafenib can cause serious side effects. See "Drug Precautions” section.

The most common side effects of regorafenib include:

• tiredness, weakness, fatigue
• loss of appetite
• frequent or loose bowel movements (diarrhea)
• swelling, pain and redness of the lining in your mouth, throat, stomach and bowel (mucositis)
• weight loss
• infection
• voice changes or hoarseness

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

Tell your healthcare provider about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take:

• carbamazepine (Carbatrol, Epitol, Equetro, Tegretol)
• clarithromycin (Biaxin)
• itraconazole (Sporanox)
• ketoconazole (Nizoral)
• nefazodone (Serzone)
• phenytoin (Dilantin, Phenytek)
• posaconazole (Noxafil)
• phenobarbital
• rifampin (Rifadin, Rifamate)
• St. John's wort
• telithromycin (Ketek)
• voriconazole (Vfend)

This is not a complete list of regorafenib drug interactions. Ask your doctor or pharmacist for more information.

Regorafenib can cause serious side effects, including:

• severe bleeding. Regorafenib can cause bleeding which can be serious and sometimes lead to death. Tell your healthcare provider if you have any signs of bleeding while taking regorafenib including: 
  • vomiting blood or if your vomit looks like coffee-grounds
  • pink or brown urine 
  • red or black (looks like tar) stools
  • coughing up blood or blood clots 
  • menstrual bleeding that is heavier than normal
  • unusual vaginal bleeding 
  • nose bleeds that happen often 
• a skin problem called hand-foot skin reaction and skin rash. Hand-foot skin reactions can cause redness, pain, blisters, bleeding, or swelling on the palms of your hands or soles of your feet. If you get this side effect or a skin rash, your healthcare provider may stop your treatment for some time.
• high blood pressure. Your blood pressure should be checked every week for the first 6 weeks of starting regorafenib. Your blood pressure should be checked regularly and any high blood pressure should be treated while you are receiving regorafenib. Tell your healthcare provider if you have severe headaches, lightheadedness, or changes in your vision. 
• decreased blood flow to the heart and heart attack. Get emergency help right away and call your healthcare provider if you get symptoms such as chest pain, shortness of breath, feel dizzy or feel like passing out.
• a condition called Reversible Posterior Leukoencephalopathy Syndrome (RPLS). Call your healthcare provider right away if you get: severe headaches, seizure, confusion, or change in vision.
• a tear in your stomach or intestinal wall (perforation).  Tell your healthcare provider right away if you get:
  • severe pain in your stomach-area (abdomen) 
  • swelling of the abdomen 
  • high fever 
• wound healing problems. If you need to have a surgical procedure, tell your healthcare provider that you are taking regorafenib. You should stop taking regorafenib at least 2 weeks before any planned surgery. 
• liver problems. Regorafenib can cause liver problems which can be serious and sometimes lead to death. Your healthcare provider will do blood tests to check your liver function before you start taking regorafenib and during your treatment with regorafenib to check for liver problems. Tell your healthcare provider right away if you get any of these symptoms of liver problems during treatment:
  • yellowing of your skin or the white part of your eyes (jaundice)
  • nausea or vomiting
  • dark “tea-colored” urine
  • change in sleep pattern

Grapefruit and grapefruit juice may interact with regorafenib and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before you take regorafenib, tell your healthcare provider if you:

• have liver problems
• have bleeding problems
• have high blood pressure
• have heart problems or chest pain
• plan to have any surgical procedures
• have any other medical conditions
• are pregnant or plan to become pregnant. Regorafenib can harm your unborn baby. Females and males should use effective birth control during treatment with regorafenib and for 2 months after your last dose of regorafenib. Tell your healthcare provider right away if you or your partner becomes pregnant either while taking regorafenib or within 2 months after your last dose of regorafenib.
• are breastfeeding or plan to breastfeed. It is not known if regorafenib passes into your breast milk. You and your healthcare provider should decide if you will take regorafenib or breastfeed. 

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Regorafenib falls into category D. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Females and males should use effective birth control during treatment with regorafenib and for 2 months after your last dose of regorafenib. Tell your healthcare provider right away if you or your partner becomes pregnant either while taking regorafenib or within 2 months after your last dose of regorafenib.

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if regorafenib passes into your breast milk. You and your healthcare provider should decide if you will take regorafenib or breastfeed.

• Take regorafenib exactly as your healthcare provider tells you.
• You will usually take regorafenib 1 time a day for 21 days (3 weeks) and then stop for 7 days (1 week). This is 1 cycle of treatment. Repeat this cycle for as long as your healthcare provider tells you to.
• Swallow regorafenib tablets whole.
• Take regorafenib at the same time each day with a low-fat breakfast.    

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), or  
• 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). 

Your healthcare provider may stop your treatment or change the dose of your treatment if you get side effects. 

• If you miss a dose, take it as soon as you remember on that day. Do not take two doses on the same day to make up for a missed dose. 
• Avoid drinking grapefruit juice and taking St. John’s Wort while taking regorafenib. These can affect the way regorafenib works. 

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your weight
• your height
• your age
• your gender

The recommended dose of regorafenib is 160 mg by mouth, once daily for the first 21 days of each 28-day cycle. Take regorafenib with food (a low-fat breakfast).

If you take too much regorafenib call your healthcare provider or go to the nearest emergency room right away.

Store regorafenib tablets at room temperature between 68° F to 77° F (20° C to 25° C).

• Keep regorafenib in the bottle that it comes in. Do not put regorafenib tablets in a daily or weekly pill box.
• The regorafenib bottle contains a desiccant to help keep your medicine dry. Keep the desiccant in the bottle. 
• Keep the bottle of regorafenib tightly closed.
• Safely throw away (discard) any unused regorafenib tablets after 28 days of opening the bottle.

WARNING: HEPATOTOXICITY