July 26, 2016
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"The U.S. Food and Drug Administration today expanded the approved use of Stivarga (regorafenib) to treat patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to other FDA-approved t"...



(regorafenib) Tablets



  • Severe and sometimes fatal hepatotoxicity has occurred in clinical trials [see WARNINGS AND PRECAUTIONS].
  • Monitor hepatic function prior to and during treatment [see WARNINGS AND PRECAUTIONS].
  • Interrupt and then reduce or discontinue Stivarga for hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis, depending upon severity and persistence [see DOSAGE AND ADMINISTRATION].


Stivarga (regorafenib) has the chemical name 4-[4-({[4-chloro-3-(trifluoromethyl) phenyl] carbamoyl} amino)-3- fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate. Regorafenib has the following structural formula:

STIVARGA® (regorafenib) Structural Formula Illustration

Regorafenib is a monohydrate and it has a molecular formula C21H15ClF4N4O3 • H2O and a molecular weight of 500.83. Regorafenib is practically insoluble in water, slightly soluble in acetonitrile, methanol, ethanol, and ethyl acetate and sparingly soluble in acetone.

Stivarga tablets for oral administration are formulated as light pink, oval-shaped tablets debossed with “BAYER” on one side and “40” on the other. Each tablet contains 40 mg of regorafenib in the anhydrous state, which corresponds to 41.49 mg of regorafenib monohydrate, and the following inactive ingredients: cellulose microcrystalline, croscarmellose sodium, magnesium stearate, povidone, and colloidal silicon dioxide. The film-coating contains the following inactive ingredients: ferric oxide red, ferric oxide yellow, lecithin (soy), polyethylene glycol 3350, polyvinyl alcohol, talc, and titanium dioxide.

What are the possible side effects of regorafenib (Stivarga)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using regorafenib and call your doctor at once if you have:

  • fever, chills, flu symptoms, mouth sores, severe or ongoing vomiting or diarrhea;
  • feeling very thirsty or hot, being unable to urinate, heavy sweating, or hot and dry skin;
  • blood in your urine or stools, coughing up blood or vomit that looks like coffee grounds;
  • heavy menstrual periods or abnormal vaginal...

Read All Potential Side Effects and See Pictures of Stivarga »

Last reviewed on RxList: 6/28/2016
This monograph has been modified to include the generic and brand name in many instances.

Report Problems to the Food and Drug Administration


You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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