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Regorafenib (Regorafenib) instructions

Common name: Regorafenib

Trade name: Regorafenib

All names: Regorafenib, Regorafenib, Regorafenib, Regorafenib, Stivarga, RES IHANCE, NUBLEXA, Regonix


Regofenib | Regorafenib is a new type of multi-kinase inhibitor that targets the generation of tumor cells, tumor angiogenesis and the maintenance of tumor microenvironment signaling by inhibiting a variety of protein kinases that promote tumor growth. Targets include: KIT, PDGFR, FGFR, BRAF, BRAFV600, RAF-1, VEGFR1/2/3, TIE-1/-2, RET.


1. Regorafenib indications:

(1). Patients with advanced metastatic colorectal cancer

Regofenib is suitable for the treatment of patients with metastatic colorectal cancer (CRC) who have previously been treated with chemotherapy regimens based on fluoropyrimidine, oxaliplatin and irinotecan (anti-VEGF therapy) and if they are KRAS wild-type (anti-EGFR therapy).


(2). Patients with gastrointestinal stromal tumors

Regofenib is used to treat patients with locally advanced, unremovable or metastatic gastrointestinal stromal tumors who have been treated with imatinib mesylate and sunitine malate.


(3). Patients with hepatocellular carcinoma

Regofenib can also be used for patients with liver cancer who have been treated with sorafenib (Nexavar).


2. Regorafenib usage and dosage:

(1). A cycle is 28 days, and in the first 21 days of each cycle, 160 mg is taken orally once a day. Continue treatment until disease progression or intolerable drug toxicity occurs.

(2). Take the medicine at the same time every day, and eat a low-fat meal (less than 60 calories, less than 30% fat) before taking the medicine. Do not take two doses on the same day.


3. Regorafenib dose adjustment:

(1) Interruption of medication: Grade 2 hand and foot skin reactions occur and recur, and cannot be relieved within 7 days even if the dosage is reduced. If grade 3 hand-foot skin reaction occurs, discontinue treatment for at least 7 days; symptomatic grade 2 hypertension; grade 3 or 4 adverse reactions.


(2) Reduce the dose to 120 mg: Grade 2 hand-foot skin reaction recurs for the first time; Grade 3 or 4 side effects have resolved; Grade 3 aspartate aminotransferase (AST)/alanine aminotransferase (ALT) is elevated, and the benefits of medication outweigh the potential risks.

(3) Reduce the dose to 80 mg: Recurrence of grade 2 hand and foot skin reactions at 120 mg dose; After recovery of grade 3 or 4 side effects at 120 mg dose;

(4) Permanent discontinuation: Unable to tolerate 80 mg gram dose; AST or ALT more than 20 times the upper limit of normal; AST or ALT more than 3 times the upper limit of normal, accompanied by bilirubin more than 2 times the upper limit of normal; AST or ALT more than 5 times the upper limit of normal after dose reduction to 120 mg; any Grade 4 adverse reaction.


4. Adverse reactions of regorafenib

The most common adverse reactions (≥30%) of regorafenib are fatigue/fatigue, reduced appetite and food intake, hand-foot skin reaction (HFSR), diarrhea, oral mucositis, weight loss, infection, hypertension and dysphonia.


5. Precautions for Regorafenib

Bleeding

Permanently discontinue Regorafenib for severe or life-threatening bleeding.


Dermatologic Toxicity

Reducing or discontinuing regorafenib depends on the severity and persistence of regorafenib dermatologic toxicity.


Hypertension

Regofenib Temporarily discontinue regorafenib or permanently discontinue regorafenib for severe or uncontrolled hypertension.


Cardiac Ischemia and Infarction

Withhold regorafenib for new or acute cardiac ischemia/infarction and resume regorafenib only after resolution of the acute ischemic event.


Reversible posterior leukoencephalopathy syndrome

Discontinue regorafenib.


Gastrointestinal perforation or fistula

Discontinue regorafenib.


Wound healing complications

Regorafenib was discontinued preoperatively and in patients with wound dehiscence.


Embryo-fetal toxicity

Regorafenib may cause fetal harm. Women are advised of the potential risks of regorafenib to the fetus.