ニンテダニブエタンスルホン酸塩

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

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 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。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

ニンテダニブエタンスルホン酸塩 価格

ニンテダニブエタンスルホン酸塩 化学特性,用途語,生産方法

• 効能

  抗線維化薬, チロシンキナーゼ阻害薬

• 商品名

  オフェブ (日本ベーリンガーインゲルハイム)

• 説明

  Nintedanib esylate is a potent, oral triple angiokinase inhibitor developed by Boehringer Ingelheim that targets proangiogenic and pro-fibrotic pathways mediated by the vascular endothelial growth factor receptor, fibroblast growth factor receptor and plateletderived growth factor receptor families, as well as Src and Flt-3 kinases. It was approved for the treatment of idiopathic pulmonary fibrosis (IPF), a condition in which the lungs become progressively scarred over time, by the US FDA in October 2014 and by the EMA in January 2015. The FDA granted nintedanib esylate fast-track, priority review, orphan product, and breakthrough designations. The drug was also approved by the EMA in November 2014 for treatment of non-small cell lung cancer in combination with docetaxel after first-line chemotherapy.

• 化学的特性

  Nintedanib esilate is a bright yellow powder. The octanol-water partition coefficient (log Pow) for the nintedanib esilate-free base was determined to be 3.6, demonstrating the molecule's lipophilic character. Due to the ionisable groups in nintedanib esilate, the lipophilicity profile is strongly pH-dependent. At physiological pH (pH = 7.4), the apparent partition coefficient (log D) was calculated to be 3.0. The molecule is less lipophilic in the acidic pH range (log D ≤ 1 for pH < 5). Nintedanib esilate is soluble in water. A saturated solution in water was found to have a concentration of 2.8 mg/mL and exhibited an intrinsic pH of 5.7. The solubility of nintedanib esilate is strongly pH dependent, with an increased solubility at acidic pH, particularly for pH < 3. The highest solubility of nintedanib esilate in organic solvents is observed in methanol and N-methylpyrrolidone. The best solubility in pharmaceutically relevant co-solvents is observed in propylene glycol. OFEV are soft gelatin capsules containing 100 mg or 150 mg nintedanib (as nintedanib esilate) for oral administration. Excipients: Each OFEV capsule contains medium-chain triglycerides, hard fat and lecithin.

• 使用

  Nintedanib Esylate is the salt form of Nintedanib, which is angiokinase inhibitor and is used in the treatment of idiopathic pulmonary fibrosis. Also inhibits the process blood vessel formation which may be used to assist in cancer therapy.

• 定義

  ChEBI: An organosulfonate salt obtained by combining nintedanib with one molar equivalent of ethanesulfonic acid. A kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and cancer.

• Properties and Applications

  Nintedanib esylate (NE) is used in the treatment of idiopathic pulmonary fibrosis (IPF) and in diverse cancers, including nonsmall cell lung cancer (NSCLC). NE has a pH-dependent solubility profile with low aqueous solubility under neutral pH and increased solubility at acidic pH. The oral bioavailability of NE is 4.7% because it is a P-gp substrate and also undergoes first-pass metabolism in the liver by esterases. However, the administration of NE along with food increases the area under the curve (AUC) and maximum concentration (Cmax) when the drug is taken with food; hence, it has a positive food effect[1].

ニンテダニブエタンスルホン酸塩 上流と下流の製品情報

ニンテダニブエタンスルホン酸塩 生産企業

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ニンテダニブエタンスルホン酸塩 スペクトルデータ(¹HNMR)

656247-18-6, ニンテダニブエタンスルホン酸塩 キーワード