How much do you know about Levomefolate calcium?

Levomefolate calcium (N-[4-[[(2-amino-1,4,5,6,7,8-hexahydro-5-methyl-4-oxo-(6S)-pteridinyl)methyl]amino]benzoyl]L-glutamic acid, calcium salt) is a synthetic calcium salt of L-5-methyltetrahydrofolate (L-5-methyl-THF), which is a metabolite of vitamin B9 and has a molecular weight of 497.5 and a molecular formula of C20H23CaN7O6 [1].

Folic acid is the man-made form of folate. Folate is a B-vitamin naturally found in some foods. It is needed to form healthy cells, especially red blood cells. Folic acid supplements may come in different forms (such as L-methylfolate, levomefolate, methyltetrahydrofolate). They are used to treat or prevent low folate levels. Low folate levels can lead to certain types of anemia. Conditions that can cause low folate levels include poor diet, pregnancy, alcoholism, liver disease, certain stomach/intestinal problems, kidney dialysis, among others. Women of childbearing age should receive adequate amounts of folic acid either through their diet or supplements to prevent infant spinal cord birth defects [2].  The calcium salt of Levomefolate calcium which belongs to the group of folate vitamins (Vitamin B9, Folacin).  It is a coenzymated form of folic acid and a more bioavailable alternative in dietary supplements [3]. 

Drug Entry: Levomefolic acid

Levomefolic acid (INN) is the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma 8. It is transported across the membranes including the blood-brain barrier into various tissues where it plays an essential role in the DNA synthesis, cysteine cycle and regulation of homocysteine, where it methylates homocysteine and forms methionine and tetrahydrofolate (THF). Levomefolate is approved as a food additive and is designated a GRAS (generally regarded as safe) compound 13. It is available commercially as a crystalline form of the calcium salt (Metafolin(R)), which has the stability required for use as a supplement 8. Supplementation of levomefolic acid is desired over folic acid due to reduced potential for masking vitamin B12 deficiency symptoms [4].

Application of Levomefolate calcium (CAS:151533-22-1)

1. mainly for folic acid antagonists (such as methotrexate, pyrimethamine, benzyl cefalexin and trimethoprim) antidote, it's usually used for prevention of methotrexate dose or overdose treatment caused severe toxic effects.

2. folic acid treatment of the following diseases, such as inflammatory diarrhea and protein-energy malnutrition (poor nutrition), pregnancy or infancy megaloblastic anemia caused by poor.

3. as adjuvant therapy for colon cancer, rectal cancer.

4. combined with 5-FU and treatment of digestive tract tumors or other 5-FU-sensitive tumors. High-dose CF used in conjunction with 5-FU (LF), the basic programme is currently the treatment of colon and rectal cancer.

5. for children with leukemia, lymphoma, and osteosarcoma, such as high dose MTX treatment when rescued [5].  

Reference

[1]https://druginformation.com/rxdrugs/D/Drospirenone-Ethinyl%20Estradiol-%20Levomefolate%20Calcium%20Tablets%20and%20Levomefolate%20Calcium%20Tablets.html
[2] https://www.webmd.com/drugs/2/drug-153831/levomefolate-calcium-oral/details
[3] https://www.alibaba.com/product-detail/Levomefolate-calcium-99-_60645947230.html
[4] https://www.drugbank.ca/salts/DBSALT001276
[5] https://www.alibaba.com/product-detail/Levomefolate-calcium-CAS-151533-22-1_60773578352.htm