Products
Regorafenib is commercially available in the form of film-coated tablets (Stivarga). It was approved in many countries in February 2013.
Structure and properties
Regorafenib (C21H15ClF4N4O3, Mr = 482.8 g/mol) is present in drugs as regorafenib monohydrate, which is practically insoluble in water.
Effects
Regorafenib (ATC L01XE21) has antitumor and antiangiogenic properties. The effects are due to inhibition of several kinases (VEGFR, TIE2, KIT, RET, RAF-1, BRAF, BRAFV600E, PDGFR, FGFR). Regorafenib has a long half-life of 20 to 30 hours. It prolonged survival in metastatic colorectal cancer by a median of 1.4 months in clinical trials.
Indications
- As a 2nd-line agent for the treatment of patients with metastatic colorectal carcinoma.
- Gastrointestinal stromal tumors, hepatocellular carcinoma (not approved in all countries).
Dosage
According to the professional information. Tablets are taken once daily at the same time after a light meal. Therapy is given in cycles with breaks in therapy (3 weeks of treatment, followed by 1 week of rest).
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Regorafenib is metabolized by CYP3A4 and UGT1A9 and is a BCRP and P-gp, UGT, and CYP inhibitor. Corresponding drug-drug interactions are possible. Another interaction has been described with antibiotics.
Adverse effects
The most common potential adverse effects include weakness, fatigue, loss of appetite, decreased food intake, hand foot syndrome, diarrhea, weight loss, infections, hypertension, and voice disorders. Regorafenib has liver-toxic properties and rarely can cause severe liver disease.
