バダデュスタット

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H373：長期にわたる、または反復暴露により臓器の障 害のおそれ

• 注意書き

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P314：気分が悪い時は、医師の診断/手当てを受けること。

  P330：口をすすぐこと。

  P501：内容物/容器を．．．に廃棄すること。

バダデュスタット 化学特性,用途語,生産方法

• 効能

  貧血治療薬, プロリン水酸化酵素阻害薬

• 説明

  Vadadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2) and HIF-PH3 (IC₅₀s = 1.1 and 0.39 micromolar, respectively). It stabilizes HIF-1α in mouse hepatocyte nuclear extracts. Vadadustat (50 and 100 mg/kg) increases erythropoietin levels in mouse serum.

• 使用

  Vadadustat is a novel HIF (Hypoxia-inducible factor) stabilizer. It provides an effective anemia treatment in nondialysis-dependent chronic kidney disease.

• 作用機序

  Vadadustat inhibits PDH and reduces the degradation of HIF-α, thereby increasing the production of endogenous erythropoietin (EPO) and improving anemia symptoms.

• 安全性

  Phase 3 clinical trials in Japan have confirmed the efficacy and safety of vadadustat for the treatment of renal anemia in patients with both non-dialysis-dependent (NDD)-chronic kidney disease (CKD) and dialysis-dependent CKD. The incidence of adverse events (AEs) and serious AEs in the vadadustat treatment group was comparable to that observed in the erythropoiesis-stimulating agents (ESA) treatment group^[2].

• 合成

  Boronic acid 69 and pyridine nitrile 70 were coupled via Suzuki coupling to give biphenyl 71. Crystallization of 71 was required to remove small amounts of undesired regioisomer coupling products. One-pot reaction: aromatic substitution with methoxy anion. Hydrolysis of the nitrile was performed simultaneously. These two independent operations were performed in one pot to give compound 72 in 92% overall yield for the two steps. Carboxylic acid 72 and amine 73 were amidated using CDI (carbodiimide) as coupling agent to give compound 74. Aluminum-mediated demethylation of 74 removed the ester and ether functionalities to give vadadustat (XI) in 84% yield.
  

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バダデュスタット スペクトルデータ(¹HNMR)

1000025-07-9, バダデュスタット キーワード