タファミジスメグルミン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H360：生殖能または胎児への悪影響のおそれ

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P281：指定された個人用保護具を使用すること。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

タファミジスメグルミン 化学特性,用途語,生産方法

• 効能

  アミロイド形成抑制薬

• 商品名

  ビンダケル (ファイザー)

• 説明

  In November 2011, the European Commission approved tafamidis meglumine (Fx-1006A, PF-06291826) for the treatment of transthyretin familial amyloid polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy. Tafamidis stabilizes both the wild type and mutant forms of TTR tetramer and prevents tetramer dissociation by noncooperatively binding to the two thyroxine binding sites. Tafamidis is the first approved medicine for TTR-FAP. The Kd values for tafamidis for the two thyroxine binding sites on TTR, as determined by isothermal titration calorimetry, were 3 nM and 278 nM, respectively. In another in vitro study using wild type TTR, V30M mutant TTR, and V122I mutant TTR, it was shown that tafamidis inhibited fibril formation in a concentration-dependent manner reaching EC₅₀ at a tafamidis:TTR stoichiometry of <1 (EC₅₀ was in the range of 2.7–3.2 μM, corresponding to a tafamidis:TTR stoichiometry range of 0.75–0.9). Tafamidis has been synthesized by coupling 4-amino-3- hydroxybenzoic acid with 3,5-dichlorobenzoyl chloride followed by dehydration using p-toluenesulfonic acid.

• 使用

  Tafamidis Meglumine is used as a potential therapeutics for COVID-19 and related viral infections

• 臨床応用

  Tafamidis meglumine is a transthyretin amyloid inhibitor that was approved for the treatment of transthyretin amyloid polyneuropathy (ATTR-PN) and transthyretin familial amyloid polyneropathy (TTR-FAP). These diseases represent a rare autosomal neurodegenerative disorder characterized by autonomic, sensory and motor impairment which are typically fatal. Tafamidis was discovered at The Scripps Research Institute and developed by Pfizer.

タファミジスメグルミン 生産企業

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