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 Levoleucovorin Calcium

L-leucovorin is the active l-isomer of the racemic mixture of the 5-formyl derivative of tetrahydrofolic acid. Metabolically active, l-leucovorin, also known levoleucovorin, does not require bioactivation by dihydrofolate reductase, an enzyme inhibited by folic acid antagonists. This agent may enhance the effects of fluoropyrimidines by stabilizing their binding to the enzyme thymidylate synthase. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

DRUG DESCRIPTION

levoleucovorin is the levo isomeric form of racemic d,l-leucovorin, present as the calcium salt. levoleucovorin is the pharmacologically active isomer of leucovorin [(6-S)-leucovorin]. levoleucovorin for injection contains levoleucovorin calcium, which is one of several active, chemically reduced derivatives of folic acid. It is useful as antidote to the inhibition of dihydrofolate reductase by methotrexate. This compound has the chemical designation calcium (6S)-N-{4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl] amino]benzoyl-L-glutamate pentahydrate. The molecular weight is 601.6. Its molecular formula is: C20H21CaN7O7 5 H2O. levoleucovorin for injection is supplied as a sterile lyophilized powder consisting of 64 mg levoleucovorin calcium pentahydrate (equivalent to 50 mg levoleucovorin) and 50 mg mannitol per 50 mg vial. Sodium hydroxide and/or hydrocholoric acid are used to adjust the pH during manufacture. It is intended for intravenous administration after reconstitution with 5.3 mL of sterile 0.9% Sodium Chloride Injection, USP

Mechanism Of Action

levoleucovorin is the pharmacologically active isomer of 5-formyl tetrahydrofolic acid. levoleucovorin does not require reduction by the enzyme dihydrofolate reductase in order to participate in reactions utilizing folates as a source of “one-carbon” moieties. Administration of levoleucovorin can counteract the therapeutic and toxic effects of folic acid antagonists such as methotrexate, which act by inhibiting dihydrofolate reductase.

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