Regorafenib
Cytostatic · Protein kinase inhibitor
Indications
Metastatic colorectal cancer previously treated with fluoropyrimidine based chemotherapy, anti-VEGF therapy and anti-EGER therapy, or when these therapies are not suitable.
Dosage
Adults: 160 mg once daily after light low-fat meal on days 1-21 of 28 day treatment cycle. Doses may be interrupted or reduced if significant adverse reactions occur. Continue treatment until benefit no longer observed or unacceptable toxicity occurs. Children: Not recommended.
Adverse Effects
Haemorrhage and serious skin reactions (discontinue if severe). Infection, thrombocytopenia, anaemia, anorexia, headache, hypertension, dysphonia, GI upset, mucosal inflammation, hyperbilirubinaemia, hand-foot skin reaction, rash, asthaenia, fatigue, pain, fever, wt loss, leucopenia, hypothyroidism, electrolyte disturbances, hyperuricaemia, tremor, taste disorders, dry mouth, GERD, dry skin, alopecia, nail disorders musculoskeletal stiffness, proteinuria, abnormal INR. Raised transaminases, amylase and lipase.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: Severe hepatic impairment. Precautions: Unstable angina, new onset angina (within 3 months), recent MI (within 6 months) or heart failure (NYHA II-IV), hypertension. History of ischaemic heart disease; monitor for myocardial ischaemia. Moderate hepatic impairment. Monitor electrolyte and metabolic parameters; interrupter discontinue if persistent or recurrent abnormalities occur. Perform LFTs before starting treatment, every 2 weeks for the first 2 months and monthly thereafter. WHO performance status >2. KRAS mutant tumours. Conditions predisposing to bleeding; monitor blood counts and coagulation parameters. Risk of reversible posterior leukoencephalopathy syndrome, gastrointestinal perforation and fistulae; discontinue if occurs. Major surgery. Ensure contraception in women and men…
Interactions
Antibacterials, bile acid sequestrants, drugs that increase bleeding risk. Strong CYP3A4 inhibitors (e.g. clarithromycin, azole antifungals, grapefruit juice) or inducers (e.g. phenytoin, carbamazepine). Strong UGT1A9 inhibitors (e.g. mefenamic acid), substrates of UGT1A9 or UGT1A1 (e.g. irinotecan).
Advice to Patient
Take with a low fat meal (<30% fat) at the same time each day. Swallow whole tablet. If you miss a dose, take it as soon as you remember unless it is time for the next dose. Contact prescriber if there is severe skin rash, chest pain, palpitations, difficulty in breathing, severe headache, change in vision, confusion, seizures, difficulty in thinking, blood in vomit, blood in cough, pink or brown urine, red or black stools, heavier menstrual bleeding, unusual vaginal bleeding, nose bleeding. Avoid taking grapefruit juice and grapefruit products during therapy. Check blood pressure every week for the first 6 weeks after starting therapy. Do not take double dose.
Pharmacokinetics
Absorption: Increased absorption with food. Bioavailability: Tab: 69%. Oral soln: 83%. Metabolism: Hepatic. Half-life elimination: 20-30 hrs. Time to peak, plasma: Approx. 3-4 hrs. Excretion: Faeces (approx. 71%). Urine (approx. 19%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
Always consult a pharmacist or doctor.