regorafenib at a glance
Medicine class
Targeted anticancer treatment and multikinase inhibitor
Licensed uses
Selected previously treated colorectal cancer, gastrointestinal stromal tumours and hepatocellular carcinoma
Taking the tablets
Swallow whole with water after a light meal containing less than 30% fat
Important monitoring
Liver function and blood pressure require close monitoring
What is regorafenib used for?
Regorafenib is licensed as monotherapy for adults in the following circumstances:
Metastatic colorectal cancer previously treated with, or unsuitable for, available therapies including fluoropyrimidine-based chemotherapy, anti-VEGF therapy and anti-EGFR therapy.
Unresectable or metastatic gastrointestinal stromal tumours that progressed during, or were intolerant of, previous imatinib and sunitinib treatment.
Hepatocellular carcinoma previously treated with sorafenib.
How does regorafenib work?
Regorafenib blocks multiple kinases, including VEGF receptors and proteins such as KIT, RAF and PDGF receptors. This can reduce tumour-cell signalling, limit formation of tumour blood vessels and hinder tumour growth and spread.
regorafenib preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg
How to take regorafenib
Follow the oncology team's prescription exactly.
Swallow the tablets whole with water.
Take them after a light meal containing less than 30% fat.
Keep the tablets in their original tightly closed bottle, with the desiccant inside, to protect them from moisture.
Tell the oncology team if swallowing whole tablets is difficult; do not alter them without advice.
regorafenib side effects
Common or expected effects
- Soreness, redness, swelling or blistering of the hands and feet
- Tiredness or weakness
- Diarrhoea, nausea, vomiting or constipation
- Reduced appetite and weight loss
- Mouth soreness or inflammation
- High blood pressure
- Pain, including abdominal or back pain
- Rash, altered voice, fever or infection
- Changes in liver tests, blood counts, electrolytes or thyroid function
Get urgent medical advice
- Possible liver injury: yellow skin or eyes, dark urine, marked tiredness, confusion or upper abdominal pain
- Severe bleeding, black stools, vomiting blood or bleeding that will not stop
- Severe abdominal pain suggesting bowel perforation or fistula
- Chest pain or other symptoms of reduced blood flow to the heart
- Seizures, severe headache, confusion or visual disturbance
- Hypertensive crisis or sudden severe abdominal, chest or back pain
- Painful widespread rash, blistering, skin peeling or mouth and eye involvement
- Severe or rapidly worsening infection
regorafenib in pregnancy
Regorafenib may harm an unborn baby and should not be used during pregnancy unless a specialist considers it clearly necessary after weighing maternal benefit against fetal risk. Effective contraception is required for people who could become pregnant and for male partners during treatment and for 8 weeks afterwards. Contact the oncology team promptly if pregnancy occurs or is planned.
regorafenib while breastfeeding
Breastfeeding must stop during regorafenib treatment because transfer into human milk is unknown and harm to infant growth and development cannot be excluded. Discuss feeding options with the oncology and maternity teams.
regorafenib interactions
Give the oncology pharmacist a complete list of prescribed, over-the-counter and herbal products. Important examples include:
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, ketoconazole, posaconazole and voriconazole
May substantially alter exposure to regorafenib and its active metabolites; concomitant use should generally be avoided.
Grapefruit juice
Can inhibit CYP3A4 and alter regorafenib exposure, so it should be avoided.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort
Can substantially alter regorafenib and active-metabolite exposure and may reduce treatment effectiveness; avoid where possible.
Common questions about regorafenib
Answers are fully visible for fast scanning and source review.
Can regorafenib tablets be crushed or chewed?
They should be swallowed whole with water. Ask the oncology team for advice if swallowing tablets is difficult rather than crushing or chewing them.
What food should regorafenib be taken with?
Take it after a light meal containing less than 30% fat. High-fat meals and fasting produce different exposure to regorafenib and its active metabolites.
Can I drink grapefruit juice while taking regorafenib?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.