Regorafenib is a multi kinase inhibitor that blocks the proliferation and spread of tumor cells by targeting various kinases related to tumor angiogenesis, tumorigenesis, and metastasis, such as VEGFR1-3, KIT, RET, PDGFR, etc.

1、 Drug name

1. Common name: Regorafenib

2. Product Name: STIVARGA ®

2、 Indications

Suitable for treating adult patients who have received corresponding standard treatments in the past:

1. Metastatic colorectal cancer (CRC).

2. Locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST).

3. Hepatocellular carcinoma (HCC, previously treated with sorafenib).

3、 Specifications

Each tablet contains 40mg of regorafenib (anhydrous equivalent to 41.49mg hydrate)

4、 Main components

Active ingredient: Regorafenib

5、 Usage and dosage

1. Recommended dosage: 160mg each time (i.e. 4 tablets 40mg), once daily, taken on the first 21 days of each 28 day cycle.

2. Usage: Take the whole tablet with a low-fat meal (with less than 600 calories and a fat content of less than 30%), and take the medication at a fixed time every day.

3. Treatment continues until disease progression or unacceptable toxicity occurs.

6、 Dose adjustment

Adjust the dosage based on the severity and duration of adverse reactions:

1. First dose reduction: After experiencing a grade 2 hand foot skin reaction (HFSR) or recovering to grade 3/4 adverse reactions (excluding infection), the dose is reduced to 120mg once daily.

2. Further reduction: If grade 2 HFSR or grade 3/4 adverse reactions occur again at a dose of 120mg (excluding hepatotoxicity or infection), the dose should be reduced to 80mg once daily.

3. Permanent discontinuation of medication: unable to tolerate a dose of 80mg; Specific severe liver toxicity indicators appear; Grade 4 adverse reactions occur (benefit risk assessment is required).

4. Suspend medication: When there are symptoms such as grade 3 HFSR, symptomatic grade 2 hypertension, grade 3/4 adverse reactions, or worsening infections, medication should be suspended.

7、 Medication precautions

1. Medication time: Take it after a low-fat meal at a fixed time every day.

2. Missing server treatment: If you remember missing a server on the same day, you should take it as soon as possible; Do not take double the dose on the same day to make up for the missed dose from the previous day.

3. Vomiting treatment: If vomiting occurs after taking medication, it should not be taken again, and treatment should continue according to the original plan for the next dose.

4. Preoperative discontinuation of medication: Discontinue medication for at least 2 weeks before elective surgery; Resume medication at least 2 weeks after major surgery and after the wound has fully healed.

5. Monitoring requirements: During the initial stage of treatment, regular monitoring of liver function, blood pressure, signs of infection, etc. is required.

8、 Medication for special populations

1. Liver dysfunction: Mild or moderate injury does not require dose adjustment; It is not recommended to use it for severe injuries (total bilirubin>3 × ULN).

2. Renal insufficiency: mild to moderate without adjustment; There is no recommended dosage for end-stage renal disease or dialysis patients.

3. Elderly individuals: Patients aged 65 and above may have a higher incidence of hypertension and require close monitoring.

4. Children: Safety and efficacy have not been established.

5. Pregnant women: There is a risk to the fetus, and they should be informed and take effective contraceptive measures.

6. Breastfeeding period: It is not recommended to breastfeed during the treatment period and within 2 weeks after the last dose.

7. Men and women of childbearing age: Effective contraceptive measures should be taken during treatment and within 2 months after the last dose.

9、 Adverse reactions

1. Common adverse reactions include pain, skin reactions on hands and feet, fatigue/weakness, diarrhea, decreased appetite, hypertension, infection, difficulty speaking, hyperbilirubinemia, fever, mucositis, weight loss, rash, nausea, etc.

2. Serious adverse reactions include: hepatotoxicity, infection, bleeding, gastrointestinal perforation or fistula, skin toxicity, hypertension, myocardial ischemia/infarction, reversible posterior leukoencephalopathy syndrome, wound healing disorders, embryo fetal toxicity, etc.

10、 Contraindications

none

11、 Drug interactions

1. Avoid co administration with strong CYP3A4 inducers as it may reduce the blood concentration of regorafenib.

2. Avoid co administration with strong CYP3A4 inhibitors as it may increase the blood concentration of regorafenib.

3. When used in combination with BCRP substrates, the toxicity risk of the latter should be closely monitored.

12、 Storage method

1. Storage temperature: 25 ℃ (77 ℉), short-term storage is allowed at 15-30 ℃ (59-86 ℉).

2. Keep the original bottle stored and do not remove the desiccant inside the bottle.

3. Tablets that have not been used up within 7 weeks after opening the bottle should be discarded.

4. Keep out of reach of children.

Regorafenibinformation