Drug intelligence / Profile preview

formyltetrahydrofolate

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Formyltetrahydrofolate is a reduced folate derivative, encompassing various isomeric forms such as 5-formyltetrahydrofolate (also known as folinic acid or leucovorin) and 10-formyltetrahydrofolate. It plays a crucial role in one-carbon metabolism, serving as a source of one-carbon units essential for key biological processes including DNA synthesis, methylation, and purine de novo synthesis. As folinic acid, it is clinically utilized to mitigate the toxic effects of antifolate drugs like methotrexate by bypassing their inhibitory action on dihydrofolate reductase. [cite: NCT00000395, 39234107, 15] It also enhances the cytotoxic activity of certain chemotherapeutic agents, such as 5-fluorouracil, by stabilizing the binding of 5-fluorodeoxyuridine monophosphate to thymidylate synthase. Its metabolism involves enzymes like ALDH1L1 and formate-tetrahydrofolate ligase.

Other names
5-formyltetrahydrofolatefolinic acidl-Leucovorin10-formyltetrahydrofolate10-formyltetrahydropteroylglutamic acidN10-formyltetrahydrofolateN-10-formyltetrahydrofolateN 10-formyltetrahydrofolate10-formyltetrahydrofolic acid
02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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