Regorafenib Side Effects

Medically reviewed by Drugs.com. Last updated on Dec 31, 2023.

Applies to regorafenib: oral tablet.

Important warnings This medicine can cause some serious health issues

Oral route (tablet)

Severe and sometimes fatal hepatotoxicity has occurred with regorafenib therapy.

Monitor hepatic function prior to and during therapy.

Adjust dose or interrupt or discontinue therapy if hepatoxicity occurs.

Serious side effects of regorafenib

Along with its needed effects, regorafenib may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking regorafenib:

More common

• bleeding gums
• bloody or cloudy urine
• blurred vision
• cough or hoarseness
• coughing up blood
• difficult, burning, or painful urination
• difficulty with breathing or swallowing
• dizziness
• fever or chills
• frequent urge to urinate
• headache
• increased menstrual flow or vaginal bleeding
• lower back or side pain
• nervousness
• nosebleeds
• painful or difficult urination
• pounding in the ears
• prolonged bleeding from cuts
• rash
• red or black, tarry stools
• redness, swelling, or pain of the skin
• scaling of the skin on the hands and feet
• slow or fast heartbeats
• tingling of the hands and feet
• ulcers on the skin

Less common

• chest pain or discomfort
• dark-colored urine
• general feeling of tiredness or weakness
• light-colored stools
• nausea or vomiting
• pain or discomfort in the arms, jaw, back, or neck
• shakiness in the legs, arms, hands, or feet
• stomach pain that continues
• sweating
• yellow eyes or skin

Rare

• blistering, peeling, or loosening of the skin
• bloody, black, or tarry stools
• chills
• confusion
• diarrhea
• heartburn
• indigestion
• itching
• joint or muscle pain
• red skin lesions, often with a purple center
• severe stomach pain, cramping, or burning
• sore throat
• sores, ulcers, or white spots in the mouth or on the lips
• trouble breathing
• unusual tiredness or weakness
• vomiting of material that looks like coffee grounds, severe and continuing

Other side effects of regorafenib

Some side effects of regorafenib may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• bad, unusual, or unpleasant taste
• hair loss or thinning of the hair
• lack or loss of strength
• muscle or joint stiffness
• weight loss

Less common

• constipation
• depressed mood
• dry skin and hair
• feeling cold
• muscle cramps
• weight gain

For healthcare professionals

Applies to regorafenib: oral tablet.

Hepatic

• Very common (10% or more): Increased AST (93%), hyperbilirubinemia (78%), increased ALT (70%)
• Common (1% to 10%): Acute kidney injury
• Uncommon (0.1% to 1%): Severe liver injury
• Frequency not reported: Hepatic failure^[Ref]

Genitourinary

• Very common (10% or more): Proteinuria (84%)
• Common (1% to 10%): Hyperuricemia^[Ref]

Hematologic

• Very common (10% or more): Anemia (79%), lymphopenia (68%), thrombocytopenia (63%), increased INR (44%), neutropenia (16%)
• Common (1% to 10%): Leukopenia^[Ref]

Metabolic

• Very common (10% or more): Hypophosphatemia (70%), hypocalcemia (59%), decreased appetite and food intake (47%), weight loss (32%), hypokalemia (31%), hyponatremia (30%), hypothyroidism (18%)
• Common (1% to 10%): Hypomagnesemia, hypoalbuminemia^[Ref]

Dermatologic

• Very common (10% or more): Hand-food skin reaction/palmar-plantar erythrodysesthesia syndrome (67%), rash (30%), alopecia (24%)
• Common (1% to 10%): Exfoliative rash, dry skin, nail disorder
• Uncommon (0.1% to 1%): Erythema multiforme
• Rare (less than 0.1%): Stevens-Johnson Syndrome, toxic epidermal necrolysis, keratoacanthoma/squamous cell carcinoma of the skin^[Ref]

Other

• Very common (10% or more): Asthenia/fatigue (64%), pain (60%), infection (32%), fever (28%), mucosal inflammation (17%)
• Common (1% to 10%): Tinnitus, ear discomfort^[Ref]

Cardiovascular

• Very common (10% or more): Hypertension (59%), hemorrhage (21%)
• Uncommon (0.1% to 1%): Myocardial ischemia, myocardial infarction, hypertensive crisis, acute coronary syndrome^[Ref]

Gastrointestinal

• Very common (10% or more): Diarrhea (47%), increased lipase (46%), mucositis (40%), increased amylase (26%), stomatitis (25%), nausea (20%), vomiting (17%)
• Common (1% to 10%): Pancreatitis, gastroesophageal reflux, gastroenteritis, dry mouth
• Uncommon (0.1% to 1%): GI fistula, GI perforation^[Ref]

Respiratory

• Very common (10% or more): Dysphonia (39%)
• Common (1% to 10%): Epistaxis^[Ref]

Nervous system

• Very common (10% or more): Headache (16%)
• Common (1% to 10%): Tremor, taste disorder, peripheral sensory neuropathy, vertigo
• Frequency not reported: Reversible posterior leukoencephalopathy syndrome/posterior reversible encephalopathy syndrome^[Ref]

Musculoskeletal

• Very common (10% or more): Muscle spasms (14%), musculoskeletal stiffness (14%)^[Ref]

Hypersensitivity

• Uncommon (0.1% to 1%): Hypersensitivity reaction^[Ref]

Further information

Regorafenib side effects can vary depending on the individual. Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Some side effects may not be reported. You may report them to the FDA.

Medical Disclaimer