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Regofenib is a multi-kinase inhibitor that blocks the proliferation and spread of tumor cells by targeting multiple kinases related to tumor angiogenesis, tumorigenesis and metastasis (such as VEGFR1-3, KIT, RET, PDGFR, etc.).
1. Generic name: Regorafenib (Regorafenib)
2. Trade name: STIVARGA
Indicated for the treatment of patients with metastatic colorectal cancer who have previously received fluorouracil, oxaliplatin and irinotecan-based chemotherapy, anti-VEGF therapy and anti-EGFR therapy (KRAS wild type).
40 mg film-coated tablets.
1. Active ingredient: regorafenib monohydrate (each tablet contains 40mg regorafenib anhydrous).
2. Excipients: microcrystalline cellulose, croscarmellose sodium, magnesium stearate, povidone, colloidal silica, etc.
1. Recommended dose : 160mg (4 tablets) orally, once a day, take for 21 consecutive days and then stop for 7 days (28 days is a cycle).
2. How to take : It needs to be taken with low-fat breakfast (fat content <30%), and the whole tablet should be swallowed. If you miss a dose, do not take it again on the same day.
1. Reduce the dose to 120mg : after the first occurrence of grade 2 hand-foot skin reaction (HFSR) or recovery of any grade 3/4 adverse reactions.
2. Reduce the dose to 80mg : Grade 2 HFSR or grade 3/4 adverse reactions (except liver toxicity) reoccurred at the 120mg dose.
3. Permanent discontinuation of : unable to tolerate 80mg dose, severe liver toxicity (such as ALT/AST>20 times the upper limit of normal) or grade 4 adverse reactions.
1. Dietary requirements : must be taken with low-fat breakfast (such as two pieces of white toast + low-fat jam + skim milk).
2. What to do if you miss a dose : Do not make up for a missed dose, and continue taking the medication as originally planned the next day.
3. Vomiting treatment : If you vomit after taking the medicine, there is no need to take more.
4. before and after surgery: Stop medication for at least 2 weeks before surgery, and then evaluate whether to resume medication after the wound heals.
1. Pregnant women : Contraindicated, may cause fetal malformation (pregnancy grade D).
2. During lactation : discontinue medication or stop breastfeeding.
3. Hepatic/renal insufficiency : No dose adjustment is required for mild to moderate hepatic insufficiency, and use is not recommended for severe hepatic insufficiency (Child-PughC).
4. U200c for the elderly: No dose adjustment is required.
1. Common (≥30%) include fatigue, decreased appetite, hand-foot skin reaction, diarrhea, stomatitis, weight loss, infection, hypertension, and hoarseness.
2. Serious adverse reactions may include liver toxicity, bleeding, gastrointestinal perforation, etc.
There are no clear absolute contraindications, but it is prohibited for those who are allergic to the drug ingredients.
1. Avoid combined use of : strong CYP3A4 inducers (such as rifampicin) or inhibitors (such as ketoconazole) may affect drug efficacy or toxicity.
2. Anticoagulant : INR needs to be closely monitored when combined with warfarin.
Save at room temperature (20-25°C), away from moisture and light, and keep the original packaging.