ベルイシグアト

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

  H301：飲み込むと有毒

  H311：皮膚に接触すると有毒

  H331：吸入すると有毒

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける 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。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P310：ただちに医師に連絡すること。

  P330：口をすすぐこと。

  P361：汚染された衣類をすべて脱ぐこと。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  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。

ベルイシグアト 化学特性,用途語,生産方法

• 効能

  血管拡張薬, グアニル酸シクラーゼ活性化薬

• 説明

  Vericiguat is a novel oral soluble guanylate cyclase (sGC) stimulator.
  - Soluble guanylate cyclase (sGC) is an enzyme that is activated by nitric oxide (NO). The activation initiates a signaling cascade which converts guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP). cGMP levels increase & protein kinase G (PKG) is activated, resulting in a decrease of intracellular free Ca++ -> vascular smooth muscle cell relaxation.
  - However, individuals with HF have reduced NO levels. Vericiguat, as a sGC stimulator, increases the enzymatic activity of sGC to generate cGMP independently of NO and enhances sGC sensitivity to endogenous NO.
  Vericiguat is the 2nd drug in this class and follows riociguat ADEMPAS, which has been approved for treating pulmonary arterial hypertension.
  SOCRATES-REDUCED was a phase II dose-finding trial of vericiguat in HF-rEF. The primary endpoint, change in NTproBNP over 12 weeks, was not statistically significant compared to placebo. A secondary exploratory analysis suggested a dose-response relationship in which higher doses of vericiguat were associated with greater reductions in NTproBNP levels.

• 使用

  Vericiguat is a novel oral soluble guanylate cyclase (sGC) stimulator that enhances the cyclic guanosine monophosphate (GMP) production pathway, by directly stimulating soluble guanylate cyclase activity, as well as sensitizing soluble guanylate cyclase to endogenous NO. It was initially developed for potential to reduce mortality and morbidity associated with chronic heart failure with reduced ejection fraction.

• 作用機序

  Vericiguat stimulates sGC, which increases cGMP production even when nitric oxide (NO) levels in the body are low. The NO-sGC-cGMP pathway is a key signaling pathway in the cardiovascular system, closely related to vasodilation, blood pressure regulation, and heart function. In patients with heart failure, this pathway may be impaired, resulting in reduced availability of NO, which in turn affects the health of the heart and blood vessels. Vericiguat helps restore the function of this pathway by mimicking the effects of NO, thereby improving the symptoms and quality of life of patients with heart failure.

• 臨床応用

  Vericiguat was advanced to clinical evaluation, as an oral therapy for chronic heart failure, either with reduced ejection fraction (HFrEF), or preserved EF (HFpEF). In mid-June 2020 Merck announced that the FDA had granted priority review status to vericiguat and based on this. The FDA approved vericiguat in January 2021, to reduce the risk of cardiovascular death, heart failure re-hospitalisation, or the requirement for outpatient intravenous diuretics, in patients with symptomatic chronic heart failure and ejection fraction less than 45%. This approval was based on efficacy data arising from the Phase 3 trial NCT02861534 (a.k.a. the VICTORIA trial).

ベルイシグアト 生産企業

Global(224)Suppliers

ベルイシグアト スペクトルデータ(¹HNMR)

1350653-20-1, ベルイシグアト キーワード