Quick Facts About: Regorafenib

Medically Reviewed by Vishal Shah, PharmD, MBA
Written by Samantha PhuaFeb 13, 20244 min read
Cancer Treatment Drugs

Source: Shutterstock.

Alternative names

Stivarga

FDA approved?

Yes, in 2012.

Used to treat

Regorafenib is used to treat metastatic colorectal cancer.

Administration and dosage

*All dosages indicated here are specific to colorectal cancer treatment.

Regorafenib is administered orally.

Regorafenib is administered in 160 mg doses once daily for 21 days of each 28-day cycle. This is applicable to patients who have been treated with previous therapies, or are not candidates for them.

If doses are missed, additional doses should not be administered on the same day to make up for it.

Treatment using regorafenib may continue until disease progression or unacceptable toxicity occurs.

Contraindications and precautions

Special precaution is required for patients with severe hepatic impairment as well as pregnancy and lactation.

Side effects

Regorafenib can cause serious or life-threatening liver problems, and immediate medical attention is required if the patient experiences:

  • Headache, confusion, change in mental status
  • Vision changes
  • A seizure
  • Pain, blisters, bleeding, or severe rash in the palms of your hands or the soles of your feet
  • Heart problems
  • Increased blood pressure
  • Perforation (a hole or tear) in your stomach or intestines
  • Severe bleeding
  • Signs of infection

Common side effects of regorafenib may include:

  • Diarrhea, nausea, stomach pain
  • Loss of appetite, weight loss
  • Increased blood pressure
  • Fever, infection
  • Abnormal liver function tests
  • Pain or redness in your mouth or throat, hoarse voice
  • Feeling weak or tired

Type of treatment

Regorafenib is a multi-kinase inhibitor.

Treatment mechanism

Regorefenib potently blocks multiple protein kinase, including kinases involved in tumor angiogenesis (VEGFR1, -2, -3), oncogenesis (KIT, RET, RAF-1, BRAF, BRAFV600E), and maintenance of the tumor microenvironment (PDGFR, FGFR).

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