Arfolitixorin (Not yet branded)

Description

Arfolitixorin is a folate analog that serves as an enhanced replacement for leucovorin (folinic acid) in colorectal cancer chemotherapy regimens. It functions as a reduced folate cofactor that potentiates the cytotoxic activity of 5-fluorouracil by stabilizing the binding of 5-FU metabolites to thymidylate synthase. Arfolitixorin is used in combination with 5-fluorouracil, oxaliplatin, and bevacizumab (FOLFOX-based regimens) for the treatment of metastatic colorectal cancer. This agent represents a next-generation folate rescue compound designed to provide more consistent and potent enhancement of fluoropyrimidine efficacy compared to standard leucovorin.

Mechanism of Action

Arfolitixorin is rapidly converted to the active reduced folate 5,10-methylenetetrahydrofolate within cancer cells. This active metabolite enhances the formation and stability of the ternary complex between fluorodeoxyuridine monophosphate (the active metabolite of 5-FU), thymidylate synthase, and the folate cofactor, leading to more effective inhibition of DNA synthesis and enhanced tumor cell death.

Molecular Targets

Side Effects

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials