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Merck

Folate Vitamin B9

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NEXT LEVEL FOLATE WITH INNOVATIVE MONOSODIUM SALT AS COUNTER-ION

Folate, also known as vitamin B9, plays an important role in many physiological functions including cell division, DNA health, and gene expression. Folate is naturally present in limited amounts in some foods, added to others, and available as a dietary supplement. Because folate is not produced by the human body, it must be consumed from dietary sources.

As an industry leader for commercial production of reduced folates, our folates both serve the nutraceutical industry as well pharmaceutical industry. Our high-quality folates are manufactured under cGMP guideline ICH Q7 and backed by dedicated regulatory support worldwide.

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A Comparison of Folate vs. Folic Acid

Folic acid, a synthetic compound not found in nature, is used in fortification and dietary supplementation programs. To be used by the body, folic acid must be metabolized via a series of conversions into 5-methyltetrahydrofolate (5-MTHF), the bioavailable form of folate found in blood. After consuming folic acid, some unmetabolized folic acid (UMFA) remains in the circulation. 5-MTHF does not cause unmetabolized folic acid (UMFA) to raise in plasma, which has been associated with the risk of cancer 1,2 and autism spectrum disorder3.

Methylfolate is a Central Alternative to Folic Acid

5-Methylfolate (5-MTHF) is the biologically active form of the B9 vitamin folate. 5-Methylfolate is directly bioavailable and therefore easy for the body to use. Folic acid is a synthetic compound not found in nature but used in fortification and dietary supplementation programs, which however entails several limitations.

To be used by the body, synthetic folic acid must be metabolized via a series of conversions into 5-MTHF, the bioavailable form necessary for the conversion of the amino acid homocysteine to essential methionine. The body uses methionine to make proteins and other important compounds4.

Methylfolate is the body’s preferred form of folate and the bodies easiest way to achieve a balanced folate intake. After all, up to 25%5 of a population may carry an MTHF polymorphism impairing them from processing folic acid provided via dietary supplements to the bioavailable form. MTHFR polymorphisms also have been linked to increased risks of several pathologies, including cancer6. For those who have this polymorphism, supplementing their diet with folic acid will be ineffective and eventually lead to critical levels of unmetabolized folic acid circulating in the body. For those and others, Methylfolate serves as a first choice and the easiest way to achieve a balanced, biologically active folate intake.

Expertise in Folates Production

With more than 70 years of expertise in high-purity folate production, we offer a complete portfolio of reduced folates for both pharmaceutical and nutritional applications. Explore our folate capabilities below and contact us to find the right folate suited for your work.

FOLATE BENEFITS

Sufficient folate levels are essential throughout life, from preconception to adulthood, to reduce the risk of growth and birth anomalies during pregnancy and to promote nervous system, cardiovascular, gastrointestinal, or bone health.

Folate insufficiency is causally related to several diseases, the most well-known of which is anemia. Low folate is also related to pregnancy complications and poor outcomes such as neural tube defects. Folate deficiency may affect growth and development of infants and children, may cause infertility in men and women, and has been related to the risk of stroke, dementia, depression, and bone fractures in the elderly, as well as cardiovascular diseases and fatty liver.


FOLATE PORTFOLIO

Arcofolin®

Arcofolin® is the latest innovation standard for folate supplementation. As the monosodium salt of L-5-methyltetrahydrofolate (L-5-MTHF) acid, Arcofolin® is the pure and crystalline form of the naturally occurring predominant form of folate.

Achieving a sufficient intake level of folate can be difficult. With large amounts of native folate being lost during processing and cooking, humans benefit from folate supplementation. Arcofolin® supplementation is critical to achieving a balanced folate intake and protecting from health risks associated with low levels of folate. When it comes to folates, with Arcofolin® - it can't get better!

Arcofolin® L-5-methyltetrahydrofolate benefits include:


Metafolin®

Metafolin® part of our portfolio of methylfolates, offers a more bioavailable alternative to folic acid in the form of our legacy manufactured calcium salt of L-5-methyltetrahydrofolic acid. Produced under cGMP conditions with high quality standards, Metafolin® has an extensive regulatory record and broad industry usage since its introduction in 2001. It fulfills the specifications of the United States Pharmacopoeia (USP).

Contact us to learn more about how bioavailable methylfolates can benefit your work in nutritional supplementation.


API Folates

Calcium Folinate / Leucovorin Calcium

Our Calcium Folinate offerings are produced under cGMP conditions with high regulatory oversight. We offer two forms of Calcium Folinate:

Calcium Folinate serve three main clinical applications:

  1. First line treatment for colorectal cancer: In combination with the anticancer drug 5- fluorouracil (5-FU), Irinotecan, Cisplatin or Oxaliplatin, and its derivatives. Calcium Folinate is a modulator of 5-FU and enhances its efficacy in cancer chemotherapy;
  2. Treatment of certain neoplastic diseases, severe psoriasis, and adult rheumatoid arthritis as a rescue therapy to reduce the toxic side effects of intermediate or high doses of methotrexate;
  3. Treatment of anemia caused by folate deficiency

Our Calcium Folinate is produced under cGMP conditions with high quality standards and fulfills specifications that are tighter than the requirement of the European or U.S. Pharmacopoeia. Furthermore, we maintain a U.S. Drug Master File (DMF), a certificate of Suitability (CEP) and a Common Technical Document (CTD) in Japan. Additional documents such as a Kosher, non-GMO, or TSE-certificate among others are also available.

Calcium Levofolinate Pentahydrate

As the first company worldwide to produce Calcium Levofolinate Pentahydrate (Levoleucovorin Calcium Pentahydrate), (6S)-5-Formytetrahydrofolic acid, Calcium Salt in commercial quantities, we are committed to delivering the highest product quality. Produced under cGMP conditions with high quality standards. Furthermore, we maintain a U.S. Drug Master File (DMF), a certificate of Suitability (CEP) and a Common Technical Document (CTD) in Japan. Additional documents such as a Kosher, non-GMO, or TSE-certificate are also available.


Folate Research Partnerships

As an industry leader for commercial production of reduced folates, we continue to evolve and innovate. We collaborate with leading research institutes and universities and support research with high-quality folates. Contact us to discuss research partnership opportunities.




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References

1.
Troen AM et al. J Nutr. 2006; 136(1): 189–94;. https://pubmed.ncbi.nlm.nih.gov/16365081/
2.
Paniz C et al. J Nutr. 2017; 147(9): 1677–1685;. https://pubmed.ncbi.nlm.nih.gov/28724658/
3.
Raghavan R et al. Am J Clin Nutr. 2020; 112(5):1304–1317;. https://pubmed.ncbi.nlm.nih.gov/32844208/
5.
Hickey SE et al. Genet Med. 2013 Feb;15(2):153. https://pubmed.ncbi.nlm.nih.gov/23288205/
6.
Petrone I et al. MTHFR C677T and A1298C Polymorphisms in Breast Cancer, Gliomas and Gastric Cancer: A Review. Genes (Basel). 2021;12(4):587. Published 2021 Apr 17. https://pubmed.ncbi.nlm.nih.gov/33920562/
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