Drug intelligence / Profile preview

folitixorin

Development stage
Phase 3
Lead developer
Fennec Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

Folitixorin is a small molecule and an active form of reduced folate developed as a biomodulator to enhance the efficacy and reduce the toxicity of fluoropyrimidine-based chemotherapy such as 5-fluorouracil (5-FU). It acts by stabilizing the covalent binding of the active metabolite of fluorouracil (FdUMP) to thymidylate synthase. This results in inhibition of thymidylate synthase activity and depletion of thymidine triphosphate (TTP), which is essential for DNA synthesis in tumor cells[1][2][3][4][6]. Folitixorin was studied primarily for use in metastatic colorectal cancer and advanced pancreatic cancer. It was granted orphan drug status for pancreatic cancer but its development has been discontinued[3][4][5].

Brand names
CoFactor
Other names
5,10-methylene-(6rs)-tetrahydrofolic acid5,10-methylene-5,6,7,8-tetrahydrofolic acid5,10-methylenetetrafolate5,10-methylenetetrahydrofolic acidfolic acid, tetrahydro-n5,n10-methylene-L-glutamic acid, n-(4-(3-amino-1,2,5,6,6a,7-hexahydro-1-oxoimidazo(1,5-f)pteridin-8(9h)-yl)benzoyl)-N5,n10-methylene-5,6,7,8-tetrahydrofolic acidN5,n10-methylenetetrahydrofolic acidN5,n10-methylenetetrahydropteroylglutamic acid
02

Targets

TS (Thymidylate synthase)

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