Drug intelligence / Profile preview

arfolitixorin + fluorouracil

Development stage
Phase 2
Lead developer
Isofol Medical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Arfolitixorin + fluorouracil is a combination chemotherapy regimen under investigation for the treatment of metastatic colorectal cancer (mCRC). Arfolitixorin is the stabilized, biologically active form of folate ([6R]-5,10-methylenetetrahydrofolate), which directly enhances the activity of fluorouracil (5-FU) by stabilizing its binding to thymidylate synthase, thereby increasing inhibition of DNA synthesis in tumor cells. Unlike leucovorin, which requires metabolic activation and has variable bioavailability, arfolitixorin acts immediately and may be particularly beneficial in patients with low folate pathway gene expression. The combination is being studied as an alternative to standard regimens using leucovorin plus 5-FU. Clinical trials have evaluated this combination both alone and with additional agents such as oxaliplatin and bevacizumab[1][3][6].

Brand names
CoFactor
Other names
arfolitixorin + 5-fluorouracilarfolitixorin + 5-FU
02

Targets

TS (Thymidylate synthase)

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