5-fluorouracil + leucovorin + regorafenib

This is a combination regimen consisting of three drugs: - 5-fluorouracil (5-FU), an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and repair. - Leucovorin (folinic acid), which enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxicity. - Regorafenib, an oral multikinase inhibitor targeting multiple protein kinases involved in tumor angiogenesis (such as VEGFR1/2/3 and TIE2), oncogenesis (including KIT, RET, RAF-1, BRAF), and the tumor microenvironment. This combination is being investigated primarily for metastatic colorectal cancer (mCRC) that has progressed after standard therapies. The regimen leverages the established backbone of fluoropyrimidine-based chemotherapy with leucovorin modulation and adds targeted inhibition via regorafenib to potentially improve disease control in refractory cases[4][8][6]. Clinical studies have shown disease control rates in heavily pretreated mCRC patients; adverse events are generally manageable with dose modifications[4][6].

Other names

5-FU + LV + regorafenib