Drug intelligence / Profile preview

levomefolate calcium

Development stage
Phase 4
Lead developer
Merck KGaA
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Levomefolate calcium is the calcium salt of L-methylfolate (levomefolic acid), the biologically active form of folate (vitamin B9) found in foods and circulating in blood. It is a small molecule drug and prescription dietary supplement used to treat or prevent folate deficiency and related conditions. Levomefolate acts as a methyl donor in one-carbon metabolism reactions essential for DNA synthesis, gene regulation, amino acid metabolism, myelin synthesis/repair, and red blood cell formation. It is the only form of folate that can cross the blood-brain barrier and serves as a cofactor for enzymes involved in monoamine neurotransmitter production (dopamine, serotonin, norepinephrine). Clinically it is used as adjunctive therapy for major depressive disorder with low serum folate levels or schizophrenia with hyperhomocysteinemia risk[4][5][6]. It also plays a role in remethylation of homocysteine to methionine via vitamin B12-dependent methionine synthase[5]. Levomefolate has been approved since 2010 for indications including acne and iron deficiency anemia[1], but its primary use today is as an adjunctive treatment for psychiatric disorders requiring dietary management of low folates.

Brand names
MetafolinDeplinCerefolin NAC
Other names
L-methylfolate calciumlevomefolic acid calcium salt(6S)-5-methyltetrahydrofolate calcium salt
02

Targets

MTR (Methionine synthase)

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