Chemical Properties
Light yellow to yellow solid
Originator
Leucovorin calcium,AstraZeneca
Definition
ChEBI: Calcium folinate is a tetrahydrofolic acid.
Manufacturing Process
5,10-Methenyl-5,6,7,8-tetrahydrofolic acid, chloride hydrochloride dihydrate
(20 g) was added in one portion to 100 ml water at 60°C followed by N,Ndiethylethanolamine (14.9 g) which adjusted the pH to 6. The mixture was
maintained at reflux for 5 hours and the pH kept between 5.7 and 6.2 by
addition of N,N-diethylethanolamine. The mixture was cooled, synthetic
magnesium silicate (15 g) added and slurried, and filtered through celite and
diluted with 40 ml SD3A (95% ethanol with 5% methanol). The filtrate was
kept at -5°C for 16 hours, aqueous calcium chloride (4.0 g) was added
dropwise to the cold filtrate, and the precipitate filtered, washed with SD3A
(100 ml) and with ethyl acetate (100 ml) and dried under reduced pressure.
Brand name
Wellcovorin (GlaxoSmithKline).
Therapeutic Function
Antidote (folic acid antagonists), Antianemic
General Description
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Biochem/physiol Actions
Folinic acid serves as a cofactor and participates in one-carbon-transfer reactions. It helps in improving wound healing in rats. Folinic acid plays a major role in children with autism to enhance verbal communication.
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.
