Regorafenib is an oral tumour deactivation agent that potently blocks multiple protein kinases, including kinases involved in tumour angiogenesis (VEGFR1, -2, -3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF, BRAFV600E), and the tumour microenvironment (PDGFR, FGFR). Regorafenib inhibits mutated KIT, a major oncogenic driver in gastrointestinal stromal tumours, and thereby blocks tumour cell proliferation.
In preclinical studies regorafenib has demonstrated antitumour activity in a broad spectrum of tumour models including colorectal and gastrointestinal stromal tumour models which is mediated by its antiangiogenic and antiproliferative effects. In addition, regorafenib has shown anti-metastatic effects in vivo. Major human metabolites (M-2 and M-5) exhibited similar efficacies compared to regorafenib in in vitro and in vivo models.
- STIVARGA is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, fluoropyrimidine-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy.
- STIVARGA is indicated for the treatment of patients with gastrointestinal stromal tumours (GIST) who have been previously treated with 2 tyrosine kinase inhibitors.
- STIVARGA is indicated for the treatment of patients with hepatocellular carcinoma (HCC) progressing on one other appropriate systemic therapy.