Drug intelligence / Profile preview

folinic acid

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Folinic acid is a chemically reduced derivative of folic acid that does not require activation by dihydrofolate reductase to be utilized by the body. It is used primarily as an antidote to counteract the toxic effects of methotrexate and other antifolate drugs (such as pyrimethamine and trimethoprim), and as an adjunct in chemotherapy regimens—most notably with 5-fluorouracil (5-FU) for colorectal cancer—to enhance antitumor efficacy. Folinic acid can also treat megaloblastic anemia due to folate deficiency when oral therapy is not possible. It may be administered orally or via intravenous or intramuscular injection[1][3][4][6]. Its mechanism involves providing a source of reduced folates for DNA synthesis and repair in healthy cells while potentiating the cytotoxic effect of fluoropyrimidines on tumor cells by stabilizing the binding of fluorodeoxyuridine monophosphate (FdUMP) to thymidylate synthase[2][7]. Folinic acid was first synthesized in 1945 and is included on the World Health Organization's List of Essential Medicines[4].

Brand names
LeucovorinCalcium Leucovorincalcium folinate
Other names
leucovorincalcium folinate5-formyl tetrahydrofolic acidcitrovorum factor
02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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