Regorafenib

Regorafenib was available in March 2017The drug was originally developed by Bayer AG in Germany and approved by the United States Food and Drug Administration (FDA) in 2012.

Subsequently, regorafenib was approved for use in Japan, the European Union and other countries and regions, and was officially launched in China in June 2017.

Regorafenib is a multi-targeted tyrosine kinase inhibitor primarily used for the treatment of metastatic colorectal cancer (mCRC).

1. Main ingredients

Regorafenib

2. Who is it for

Patients with colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma who have received certain treatments in the past.

3. Use in a specific group of people

【Pregnant women】

Pregnant women are advised not to use this medicine

【Lactating women】

Lactating women are advised not to breastfeed during treatment with regorafenib and for 2 weeks after the last dose

【Males and females of reproductive potential】

Women of reproductive potential are advised to use effective non-hormonal contraceptives during treatment with regorafenib and for 2 months after the last dose. Men with female partners of reproductive potential are advised to use effective contraception during treatment with regorafenib and for 2 months after the last dose

The safety and efficacy of in pediatric patients have not been established

There is no significant difference in elderly patients, and it is used under the guidance of a doctor

【Patients with liver impairment】

Patients with mild to moderate liver injury do not need to adjust the dose, and patients with severe liver injury are not recommended to use this product

【Patients with renal impairment】

Patients generally do not need to adjust the dose, and there is no recommended dose for patients with renal impairment

4. Overdose

There is no known antidote to regorafenib overdose. In cases of suspected overdose, regorafenib is discontinued and treated supportively until clinically stable

5. Storage

Store at 20 °C-25 °C; Shipping is allowed at temperatures of 15°C-30°C

6. Pharmacokinetics

After a single dose of 160 mg of regorafenib in patients with advanced solid tumors, regorafenib reached a geometric mean peak plasma level (Cmax) of 2.5 μg/mL in a median time of 4 hours, and the geometric mean area (AUC) under the plasma concentration versus time curve was 70.4 μg*h/mL

afenib was approved for use in Japan, the European Union and other countries and regions, and was officially launched in China in June 2017.

from FDA，2020.02