Levomefolic acid/ja: Difference between revisions

Levomefolic acid/ja
Created page with "<small>L</small>-メチル葉酸は水溶性で、主に腎臓から排泄される。冠動脈疾患を持つ21人の被験者を対象とした研究では、経口または非経口投与後1~3時間で血漿中濃度のピークに達した。ピーク濃度は葉酸の7倍以上高いことがわかった(129 ng/ml対14.1 ng/ml)。"
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Created page with "2012年9月、同じ3人の原告は、国際貿易委員会が同じ4人の被告に対して{{uscsub|19|1337|}}調査を開始するよう要求する訴状を提出した。訴状によれば、グノーシスの「エクストラフォリック-S」とそれを原料とする製品は、3つの特許を侵害しているという: {{patent|US|5997915}}、{{patent|US|6673381}}、{{patent|US|7172778}}である。"
 
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{{Anchor|Metabolism}}
{{Anchor|Metabolism}}


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[[File:MTHFR metabolism.svg|center|thumb|650px|MTHFR代謝:葉酸サイクル、メチオニンサイクル、トランス-硫酸化、[[hyperhomocysteinemia/ja|高ホモシステイン血症]][[5-MTHF/ja|5-MTHF]]5-メチルテトラヒドロ葉酸;5,10-メチルテトラヒドロ葉酸;[[Bcl-2-associated X protein/ja|BAX]]Bcl-2関連Xタンパク質; [[BHMT/ja|BHMT]]: ベタイン-ホモシステインS-メチルトランスフェラーゼ; [[cystathionine beta synthase/ja|CBS]]: シスタチオニンβ合成酵素; [[cystathionine gamma-lyase/ja|CGL]]: シスタチオニンγリアーゼ; [[dihydrofolate/ja|DHF]]: ジヒドロ葉酸(ビタミンB9);[[dimethylglycine/ja|DMG]]:ジメチルグリシン;[[dTMP/ja|dTMP]]:チミジン一リン酸;[[dUMP/ja|dUMP]]:デオキシウリジン一リン酸;[[flavin adenine dinucleotide/ja|FAD]]<sup>+</sup>フラビンアデニンジヌクレオチド;[[10-formyltetrahydrofolate/ja|FTHF]]10-ホルミルテトラヒドロ葉酸;[[methionine synthase/ja|MS]]:メチオニン合成酵素;[[MTHFR/ja|MTHFR]]:メチレンテトラヒドロ葉酸還元酵素;[[S-アデノシル-L-ホモシステイン|SAH]]S-アデノシル-L-ホモシステイン;[[S-adenosyl-L-homocysteine/ja|SAME]]S-アデノシル-L-メチオニン;[[tetrahydrofolate/ja|THF]]:テトラヒドロ葉酸。]]
[[File:MTHFR metabolism.svg|center|thumb|650px|MTHFR metabolism: folate cycle, methionine cycle, trans-sulfuration and [[hyperhomocysteinemia]]. [[5-MTHF]]: 5-methyltetrahydrofolate; 5,10-methyltetrahydrofolate; [[Bcl-2-associated X protein|BAX]]: Bcl-2-associated X protein; [[BHMT]]: betaine-homocysteine S-methyltransferase; [[cystathionine beta synthase|CBS]]: cystathionine beta synthase; [[cystathionine gamma-lyase|CGL]]: cystathionine gamma-lyase; [[dihydrofolate|DHF]]: dihydrofolate (vitamin B9); [[dimethylglycine|DMG]]: dimethylglycine; [[dTMP]]: thymidine monophosphate; [[dUMP]]: deoxyuridine monophosphate; [[flavin adenine dinucleotide|FAD]]<sup>+</sup> flavine adenine dicucleotide; [[10-formyltetrahydrofolate|FTHF]]: 10-formyltetrahydrofolate; [[methionine synthase|MS]]: methionine synthase; [[MTHFR]]: methylenetetrahydrofolate reductase; [[S-adenosyl-L-homocysteine|SAH]]: S-adenosyl-L-homocysteine; [[S-adenosyl-L-methionine|SAME]]: S-adenosyl-L-methionine; [[tetrahydrofolate|THF]]: tetrahydrofolate.]]
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==医療用途==
==Medical uses==
{{Anchor|Medical uses}}
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=== 大うつ病性障害 ===
=== Major depressive disorder ===
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研究によると、レボメ葉酸 (<small>L</small>-メチル葉酸) は、治療効果が得られないか、[[Selective serotonin reuptake inhibitor/ja|SSRI]] [[Serotonin–norepinephrine reuptake inhibitor/ja|SNRI]]による治療効果が一部に限られる場合の一部の患者に対して、[[First line agent/ja|第一選択]][[antidepressant/ja|抗うつ薬]][[adjunctive therapy/ja|併用]]して用いると、穏やかな抗うつ効果が認められた。レボメ葉酸は、[[Atypical antipsychotic/ja|第二世代抗うつ薬]] (非定型抗精神病薬) と比較して、併用療法として費用対効果が高い可能性がある。
Research suggests that levomefolic acid (<small>L</small>-methylfolate) taken with a [[First line agent|first-line]] [[antidepressant]] provides a modest [[Adjunctive therapy|adjunctive]] antidepressant effect for individuals who do not respond or have only a partial therapeutic response to [[Selective serotonin reuptake inhibitor|SSRI]] or [[Serotonin–norepinephrine reuptake inhibitor|SNRI]] medication, and might be a more cost-effective adjunctive agent than [[Atypical antipsychotic|second-generation antipsychotics]].
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=== 心血管疾患と癌 ===
=== Cardiovascular disease and cancer ===
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レボメ葉酸(および葉酸)は、心血管疾患および乳がんや[[colorectal cancer/ja|大腸がん]]などの進行がんの治療薬として提案されている。葉酸は体内のいくつかの代謝段階を迂回し、薬物[[fluorouracil/ja|フルオロウラシル]]の代謝産物である[[FdUMP/ja|FdUMP]][[thymidylate synthase/ja|チミジル酸合成酵素]]をよりよく結合させる。
Levomefolic acid (and folic acid in turn) has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and [[colorectal cancer]]s. It bypasses several metabolic steps in the body and better binds [[thymidylate synthase]] with [[FdUMP]], a metabolite of the drug [[fluorouracil]].
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==特許問題==
==Patent issues==
{{Anchor|Patent issues}}
In March 2012, [[Merck KGaA|Merck & Cie]] of [[Switzerland]], [[Pamlab]] LLC (maker of [[Metanx]] and [[Cerefolin]], Neevo DHA, and Deplin), and South Alabama Medical Science Foundation (SAMSF) (the plaintiffs) filed a complaint in the [[United States District Court for the Eastern District of Texas]] against four defendants: Macoven Pharmaceuticals (owned by Pernix Therapeutics), Gnosis SpA of Italy, Gnosis U.S.A and Gnosis Bioresearch Switzerland. The plaintiffs alleged that the defendants infringed on several of the plaintiffs' patents. The Macoven products named in the suit are: "Vitaciric-B", "ALZ-NAC", "PNV DHA", and l-methylfolate calcium (levomefolate calcium).
2012年3月、[[:ja:スイス|スイス]]の[[:en:Merck KGaA|Merck & Cie]][[:en:Pamlab|Pamlab]] LLC([[:en:Metanx|Metanx]][[:en:Cerefolin|Cerefolin]]、Neevo DHA、およびDeplinの医薬品メーカー)、およびSouth Alabama Medical Science Foundation(SAMSF)(原告)は、4人の被告に対して[[:en:United States District Court for the Eastern District of Texas|テキサス州東部地区連邦地方裁判所]]に訴状を提出した: Macoven Pharmaceuticals社(Pernix Therapeutics社所有)、Gnosis SpA社(イタリア)、Gnosis U.S.A.社、Gnosis Bioresearch Switzerland社である。原告側は、被告らが原告側の複数の特許を侵害していると主張した。訴訟で名指しされたマコベン製品は以下の通りである: Vitaciric-B」、「ALZ-NAC」、「PNV DHA」、「l-メチル葉酸カルシウム(レボメ葉酸カルシウム)」である。
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2012年9月、同じ3人の原告は、[[:en:United States International Trade Commission|国際貿易委員会]]が同じ4人の被告に対して{{uscsub|19|1337|}}調査を開始するよう要求する訴状を提出した。訴状によれば、グノーシスの「エクストラフォリック-S」とそれを原料とする製品は、3つの特許を侵害しているという: {{patent|US|5997915}}{{patent|US|6673381}}{{patent|US|7172778}}である。
In September 2012, the same three plaintiffs filed a complaint requesting that the [[United States International Trade Commission|International Trade Commission]] begin a {{uscsub|19|1337|}} investigation of the same four defendants. The complaint states that Gnosis' "Extrafolic-S" and products which are made from it, infringe upon three of their patents: {{patent|US|5997915}}, {{patent|US|6673381}}, and {{patent|US|7172778}}.
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==製剤==
==Formulations==
レボメ葉酸カルシウムは、レボメ葉酸のカルシウム[[salt (chemistry)/ja|]]であり、メタフォリンという商品名で販売され、デプリンに配合されている。レボメ葉酸マグネシウムはレボメ葉酸のマグネシウム塩であり、エンライテの主成分であるデルタ葉酸として製造されている。
Levomefolate calcium, a calcium [[salt (chemistry)|salt]] of levomefolic acid is sold under the brand name Metafolin and incorporated in Deplin. Levomefolate magnesium is a magnesium salt of levomefolic acid, manufactured as DeltaFolate, a primary ingredient in EnLyte.
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== こちらも参照 ==
== See also ==
* [[5,10-Methylenetetrahydrofolate/ja]]  
* [[5,10-Methylenetetrahydrofolate]]  
* [[S-Adenosylmethionine/ja]] (SAMe)
* [[S-Adenosylmethionine]] (SAMe)
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== 外部リンク ==
== External links ==
*[http://www.fao.org/docrep/008/a0044e/a0044e05.htm#bm5.3 Calcium L5-methyltetrahydrofolate (L-5-MTHF-Ca)]
*[http://www.fao.org/docrep/008/a0044e/a0044e05.htm#bm5.3 Calcium L5-methyltetrahydrofolate (L-5-MTHF-Ca)]
* {{cite journal | vauthors = Brockton NT | title = Localized depletion: the key to colorectal cancer risk mediated by MTHFR genotype and folate? | journal = Cancer Causes & Control | volume = 17 | issue = 8 | pages = 1005–16 | date = October 2006 | pmid = 16933051 | doi = 10.1007/s10552-006-0051-5 | s2cid = 20394873 }}
* {{cite journal | vauthors = Brockton NT | title = Localized depletion: the key to colorectal cancer risk mediated by MTHFR genotype and folate? | journal = Cancer Causes & Control | volume = 17 | issue = 8 | pages = 1005–16 | date = October 2006 | pmid = 16933051 | doi = 10.1007/s10552-006-0051-5 | s2cid = 20394873 }}
* {{cite journal | vauthors = Stahl SM | title = Novel therapeutics for depression: L-methylfolate as a trimonoamine modulator and antidepressant-augmenting agent | journal = CNS Spectrums | volume = 12 | issue = 10 | pages = 739–44 | date = October 2007 | pmid = 17934378 | doi = 10.1017/S1092852900015418 | s2cid = 27000937 }}
* {{cite journal | vauthors = Stahl SM | title = Novel therapeutics for depression: L-methylfolate as a trimonoamine modulator and antidepressant-augmenting agent | journal = CNS Spectrums | volume = 12 | issue = 10 | pages = 739–44 | date = October 2007 | pmid = 17934378 | doi = 10.1017/S1092852900015418 | s2cid = 27000937 }}
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{{Vitamin/ja}}
{{Vitamin}}
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{{二次利用|date=27 February 2024}}
[[Category:Folates]]
[[Category:Folates]]
[[Category:Coenzymes]]
[[Category:Coenzymes]]
[[Category:Medical food]]
[[Category:Medical food]]
[[Category:Patent case law]]
[[Category:Patent case law]]
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