antianemic, antidote to folic acid antagonists. Calcium folinate (folinic acid, calcium leucovorin, tetrahydrofolate) can be used in the management of methotrexate overdose and to reduce the toxicity of high-dose methotrexate chemotherapy.Calcium folinate is a reduced form of folic acid, which bypasses the inhibition of dihydrofolate reductase by methotrexate.Calcium folinate also has a role in combination with fluorouracil in the treatment of bowel cancer, where its use enhances the effect of fluorouracil by inhibition of thymidilate synthase.
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Mechanism of action
The mechanism of action of Calcium folinate against cancer is to stabilise the complex between 5-FU and thymidylate synthase, thereby enhancing the cytotoxicity of 5-FU, a pyrimidine analogue and inhibitor of thymidylate synthase, which blocks DNA production. Thymidylate synthase converts deoxyuridine monophosphate to thymine monophosphate. Administration of 5-FU reduces deoxythymidine monophosphate, preventing DNA synthesis and leading to cell death.
