Target intelligence / Profile preview

Levomefolic acid (L-5-methyltetrahydrofolate) (L-5-MTHF)

Target
L-5-MTHF
Molecular classification
Other (active vitamin/coenzyme; not a receptor or enzyme)
01

Overview

L-5-methyltetrahydrofolate, also known as levomefolic acid, is the **predominant active form of folate used directly by cells**. It is vital for methyl group donation in the conversion of homocysteine to methionine, supporting DNA synthesis, repair, and neurotransmitter production. It is especially critical during periods of rapid cell division, such as embryonic development, and is the main circulating form of folate capable of crossing the blood-brain barrier[1][2][6][10]. Supplementation is beneficial for individuals with genetic variants affecting folate metabolism, most notably the MTHFR gene[8][6]. L-5-methyltetrahydrofolate is not itself a classical drug target, but is a metabolite and coenzyme necessary for multiple cellular reactions, and its deficiency or altered handling is associated with diseases ranging from cardiovascular to neurodevelopmental disorders[2][4][8][10].

Other names
L-methylfolate(6S)-5-methyltetrahydrofolate(6S)-5-MTHF5-MTHF5-methyl-THFN5-methylfolateCalcium L-5-methyltetrahydrofolateLevomefolate calciumDeplin
02

Mechanism of action

Provides methyl groups for methylation reactions; Promotes homocysteine conversion to methionine

03

Biological functions

Methylation of homocysteine to methionineDNA synthesis and repairSynthesis of purines and thymidineNeurotransmitter synthesisRegulation of homocysteine
04

Disease associations

Neural tube defects (prevention)Cardiovascular disease (homocysteine management)Major depressive disorder (adjunctive therapy)Psychiatric disease (some evidence in depressive and cognitive symptoms)Folate deficiency syndromes
05

Safety considerations

May mask vitamin B12 deficiency, leading to neurological complicationsInteractions or supplementation should be monitored in those with MTHFR polymorphisms
06

Interacting drugs

Folic acid (precursor, not direct interaction)

3 more in the full profile.

07

Biomarkers

Plasma homocysteine (indirect marker of 5-MTHF status)Serum folate and vitamin B12

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