Regorafenib is an oral multi-kinase inhibitor that targets multiple tumor signaling pathways. With a broad spectrum of targets, it inhibits both the VEGF pathway and its bypass mechanisms, effectively disrupting inter-pathway crosstalk. This deep blockade helps overcome resistance to anti-angiogenic therapies, modulates the tumor immune microenvironment, and delays tumor progression. It is used for the treatment of: ① Metastatic colorectal cancer (mCRC) in patients who have previously received chemotherapy based on fluorouracil, oxaliplatin, and irinotecan, or who have previously received or are unsuitable for anti-VEGF and anti-EGFR therapy (RAS wild-type); ② Locally advanced, unresectable, or metastatic gastrointestinal stromal tumors (GIST) in patients who have previously received imatinib mesylate and sunitinib malate; ③ Hepatocellular carcinoma (HCC) patients who have previously been treated with sorafenib. Regorafenib has received high-level evidence-based recommendations from various authoritative guidelines, including those from the Chinese Society of Clinical Oncology (CSCO), the National Comprehensive Cancer Network (NCCN), and the European Society for Medical Oncology (ESMO).

Kegora® Regorafenib Tablets were approved for market in August 2024, offering more treatment options for tumor patients. It can be used as a first-line treatment for metastatic colorectal cancer, hepatocellular carcinoma, and advanced or metastatic gastrointestinal stromal tumors.