Regorafenib
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Molecule Summary
| Uses | Colorectal, Liver And Gastrointestinal Stromal Tumours |
| Therapy | Anti-Neoplastic |
| Side Effects | Hand-Foot Skin Reaction, Tiredness, Diarrhoea, High Blood Pressure |
Assurance
available
Regulated
Molecule Description
Regorafenib is an anti-cancer medicine that contains regorafenib. Regorafenib belongs to a class of medicines called kinase inhibitors. It is used treat certain advanced cancers, including metastatic colorectal cancer, and hepatocellular carcinoma (HCC) in patients previously treated with sorafenib.
Regorafenib blocks proteins (kinases) that tumour cells use to grow, spread, and build the blood vessels (angiogenesis).
Regorafenib can cause severe liver damage. Your doctor will monitor your liver function before you start and regularly during treatment. Inform your doctor immediately if you notice yellowing of your skin or eyes, dark urine, unusual tiredness, or nausea and vomiting.
Regorafenib is taken as prescribed by your doctor with a low-fat meal.
Regorafenib can cause side effects like severe bleeding, a tear in the stomach or bowel wall, severe skin reactions, high blood pressure, reduced blood flow to the heart, and delayed wound healing. Tell your doctor immediately if you notice symptoms like unusual bleeding or bruising, severe stomach pain, chest pain, or skin blistering.
Before starting treatment, inform your doctor about any liver problems, bleeding disorders, high blood pressure, heart problems, or plans for surgery. Use effective contraception during treatment and avoid breastfeeding while on Regorafenib treatment.
Uses
- To treat certain advanced cancers, including metastatic colorectal cancer, and hepatocellular carcinoma (HCC) in patients previously treated with sorafenib.
Contraindications
When should one not use Regorafenib
- Regorafenib should not be used in patients with known hypersensitivity to regorafenib or any ingredient in the medicine.
Side effects
Common side effects of this drug are:
- Pain (especially in the stomach area )
- Hand-foot skin reaction (redness, pain, blisters on palms/soles)
- Tiredness and weakness, headache, dizziness
- Diarrhoea, nausea
- Decreased appetite
- High blood pressure
- Infections
- Voice changes or hoarseness
- Fever, weight loss, rash, mouth sores (mucositis)
- Raised liver enzymes and bilirubin
- Cough, shortness of breath
- Bleeding episodes
- Low platelet, white cell, and red cell counts in blood reports
- Severe liver damage with symptoms like yellowing of skin/eyes, dark urine, nausea, vomiting
- Severe bleeding
- Sudden severe stomach pain, swelling, fever, chills (possible tear in the stomach or bowel wall)
- Severe skin blistering or peeling
- Uncontrolled high blood pressure, severe headache, vision changes
- Chest pain, shortness of breath, feeling faint
- Severe headache, seizures, confusion, vision changes
- Wound healing problems after surgery
Precautions and Warnings
Pregnancy
Breast Feeding
Driving
Alcohol
Other General Warnings
Talk to your doctor if
- Consult your doctor:
- If you have any liver disease.
- If you have a history of bleeding problems.
- If you have uncontrolled high blood pressure or a heart condition.
- If you have had a recent infection or wound that has not healed.
- If you have plans for surgery, current or upcoming.
- Report any signs of liver problems, unusual bleeding, or severe abdominal pain to your doctor immediately.
- Attend all scheduled liver-function tests and blood pressure checks, especially in the first weeks of treatment.
- Diarrhea may occur as a side effect. Drink plenty of fluids and inform your doctor if it doesn't stop or if you find blood in your stools.
- Monitor your blood pressure regularly while taking this medication. Inform your doctor if you notice symptoms of very high blood pressure such as severe headache, confusion, problems with your eyesight, nausea or vomiting.
- Tell your doctor about all other medicines and supplements you take.
- Keep out of the sight and reach of children and pets at all times.
Mode of Action
How Does It Work?
Regorafenib belongs to a class of medicines called kinase inhibitors. It blocks several kinase proteins involved in tumour growth, tumour blood vessel formation, and spread of cancer cells, which helps slow or stop tumour growth.
Interactions
Interactions with other medicines
- Regorafenib can interact with some medicines, changing how they work or increasing the risk of side effects.
- Some antifungal and antibiotic medicines: Clarithromycin, itraconazole, ketoconazole, posaconazole, and voriconazole may increase regorafenib levels. These medicines should generally be avoided unless your doctor advises otherwise.
- Some painkillers: Mefenamic acid, diflunisal, and niflumic acid may affect regorafenib levels and should generally be avoided during treatment.
- Certain medicines such as methotrexate, fluvastatin, and atorvastatin: Regorafenib may increase their levels and the risk of side effects. Your doctor may monitor you more closely.
- Warfarin and other blood thinners: Regorafenib may increase the risk of bleeding. Your doctor may recommend closer monitoring.
- Tell your doctor about all prescription and over-the-counter medicines, vitamins, supplements, and herbal products you take before starting regorafenib.
Interactions with food items
Take Regorafenib after a low-fat meal. Avoid high-fat meals around the time you take the medicine, as they can affect how much regorafenib your body absorbs Regorafenib.
Dosage
Overdose
No specific antidote for Regorafenib overdose is available. If an overdose is taken or suspected, seek urgent medical attention immediately.
Missed a Dose
If you miss a dose, take it the same day as soon as you remember. Do not take two doses on the same day to make up for a missed dose from the day before. If you are ever unsure whether you took a dose, contact your doctor for guidance.
Frequently Asked Questions (FAQs)
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References:
- DailyMed. Regorafenib prescribing information. 2026 [Cited 17th Sep 2026]
- electronic medicines compendium (emc). Regorafenib Summary of Product Characteristics. 2026 [Cited 17th Sep 2026]
- Central Drugs Standard Control Organisation (CDSCO). Drugs@CDSCO [Internet]. New Delhi: Directorate General of Health Services, Ministry of Health & Family Welfare, Government of India. 2026 [Cited 17th Sep 2026]
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