arfolitixorin

Arfolitixorin is a stabilized and biologically active pure form of folate ([6R]-5,10-methylenetetrahydrofolate), developed as a biomodulator to enhance the efficacy of 5-fluorouracil (5-FU)–based chemotherapy in advanced colorectal cancer. Unlike leucovorin or levoleucovorin, which require metabolic activation to become effective in the body, arfolitixorin is immediately active and can be used regardless of patients' genetic ability to convert prodrugs into the active form. Its mechanism involves increasing intracellular levels of methylenetetrahydrofolate in tumor cells, thereby enhancing thymidylate synthase inhibition by 5-FU and leading to persistent DNA synthesis arrest and tumor cell death through apoptosis. Arfolitixorin has been studied primarily for metastatic colorectal cancer (mCRC), with ongoing clinical trials including a global phase III study. The drug was granted FDA fast track designation for advanced colorectal cancer due to its potential to address unmet medical needs[1][3][5][7][8].

Brand names

modufolin

Other names

(6R)-5,10-methylenetetrahydrofolic acidL-(+)-methylenetetrahydrofolic acid