トファシチニブクエン酸塩

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

  H315：皮膚刺激

  H319：強い眼刺激

• 注意書き

  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。

  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。

  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。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

トファシチニブクエン酸塩 価格

トファシチニブクエン酸塩 化学特性,用途語,生産方法

• 用途

  強力な JAK 阻害剤です（IC50=1 nM（JAK3），20 nM（JAK2），112 nM（JAK1））。

• 用途

  強力な JAK 阻害剤です（IC50=1 nmol/l（JAK3），20 nmol/l（JAK2），112 nmol/l（JAK1））。

• 効能

  抗リウマチ薬, ヤヌスキナーゼ(JAK)阻害薬

• 商品名

  ゼルヤンツ (ファイザー)

• 説明

  Tofacitinib citrate, also known as CP-690550 citrate, is a king of drugs developed by the US pharmaceutical company Pfizer for treating rheumatoid arthritis, trade name Xeljanz, for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid arthritis (RA) in adult patients. This product is a Janus kinase inhibitor, administered twice daily.
  November 6, 2012, the US Food and Drug Administration (FDA) and Pfizer jointly announced Tofacitinib citrate is approved for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid joints arthritis (RA) in adult patients.
  Xeljanz can be used as monotherapy or in combination with methotrexate or other non-biological disease-modifying antirheumatic drugs (the DMARD) in combination. This medicine should not be in combination with biological DMARD or strong immunosuppressants (such as cyclosporine and azathioprine). Xeljanz is approved by the daily dose of 2 times, each time 5mg.
  Seven clinical trials evaluated the safety and efficacy of Tofacitinib citrate in moderate to severe active RA in adult patients. In all tests, compared with patients receiving placebo, patients receiving Xeljanz treatment showed significant improvement in clinical response and physical function.
  In Clinical trials, the most common adverse events were upper respiratory tract infection, headache, diarrhea, nasal congestion, sore throat, and nasopharyngitis.
  Using Xeljanz was associated with an increased risk of serious infections, including opportunistic infections, tuberculosis, cancer and lymphoma. Xeljanz product label attaches boxed warning on these security risks. Xeljanz treatment is also associated with reducing blood cell counts and increasing cholesterol and liver enzyme values.
  In order to study Xeljanz long-term impact on heart disease, cancer and severe infections, FDA requires for a post-marketing study, which will evaluate two doses of Xeljanz (Tofacitinib citrate) therapy, and accept a integration of another group of patients approved by the treatment as a control.

• 使用

  Tofacitinib citrate has been used:
  as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studies
  as a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan loss
  as a Janus kinase inhibitor in MCF7 breast cancer cells

• 定義

  ChEBI: Tofacitinib citrate is a citrate salt obtained by combining equimolar amounts of tofacitinib and citric acid. Used to treat moderately to severely active Rheumatoid Arthritis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antirheumatic drug. It contains a tofacitinib.

• 一般的な説明

  Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.

• 副作用

  The most common side effects of Tofacitinib citrate are upper respiratory tract infection, headache, diarrhoea and nasopharyngitis. Other side effects that may occur are increased risk of infections (tuberculosis, hepatitis B, hepatitis C, herpes zoster), higher cholesterol levels, heart disease, stroke and blood clots. Very rare side effects are perforation of the colon, lymphoma and other malignancies.

• 代謝

  70% metabolised in the liver by CYP3A4 (major) and CYP2C19 (minor). The 8 metabolites produced are inactive.

• 参考文献

  1. The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis. PMID: 26966791
  2. Binding of Janus kinase inhibitor tofacitinib with human serum albumin: multi-technique approach DOI:10.1080/07391102.2015.1104522
  3. Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo. DOI:10.1016/j.bcp.2018.07.034
  4. Phosphoproteome profiling reveals critical role of JAK-STAT signaling in maintaining chemoresistance in breast cancer DOI:10.18632/oncotarget.21801
  5. Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34 DOI:10.1016/j.tips.2010.10.004
  6. http://www.medicinenet.com/tofacitinib_citrate_xeljanz/article.htm

トファシチニブクエン酸塩 生産企業

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トファシチニブクエン酸塩 スペクトルデータ(¹HNMR)

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