タクロリムス

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

  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

  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。

  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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P310：飲み込んだ場合：直ちに医師に連絡すること。

タクロリムス 価格

タクロリムス 化学特性,用途語,生産方法

• 外観

  白色〜ほとんど白色, 結晶〜粉末

• 溶解性

  アセトニトリルに溶ける。

• 用途

  強 力 な 免疫抑制剤 で す。 FK506はFK506結合タンパク-12（FKBP12） と複合体を形成し、さらにカルシニューリン に結合し、IL-2、インターフェロンに代表さ れる種々のサイトカインの発現を抑制しま す。これにより細胞外性 T 細胞の分化増殖を 抑制します。

• 効能

  抗アレルギー薬, 免疫抑制薬, カルシニューリン阻害薬

• 説明

  Tacrolimus, isolated from the microorganism Streptomyces tsukubaensis, is a macrolide immunosuppressant developed by Fujisawa for organ transplantation. It displays similar but more potent immunosuppressive activity than cyclosporin. It inhibits both cell mediated and humoral immune responses. In animal models of organ transplantation, tacrolimus has been shown to prolong survival of hepatic, renal, cardiac, small intestine, pancreatic and skin allografts and to reverse cardiac and renal allograft rejection. It has been used effectively in humans as rescue or primary immunosuppressant therapy in liver or kidney transplantation. Compared to cyclosporin, tacrolimus causes reduced incidence of infectious complications and of hypertension and hypercholesterolemia for the allograft recipients. In common with cyclosporin, tacrolimus binds with high affinity to a family of cytoplasmic immunosuppressant binding proteins, the immunophilins. This tight complex is proposed as the biologically active moiety that interacts with intracellular molecules involved in signal transduction.It inhibits phosphatase activity of calcineurin, an action that may impair the generation and/or activation of nuclear transcription factors required for lymphokine (particularly interleukin-2) gene expression. Tacrolimus has also been reported to have potential in multiple sclerosis, psoriasis, rheumatoid arthritis and uveitis associated with Behcet‘s disease.

• 化学的特性

  White Crystalline Solid

• 使用

  FK-506 (Tacrolimus) is a macrolide immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system

• 定義

  ChEBI: Tacrolimus is a macrolide containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.

• 適応症

  Tacrolimus is a macrolide lactone originally derived from Streptomyces tsukubaensis. Although structurally unrelated to cyclosporine, tacrolimus has a very similar mechanism of action; that is, it blocks the production of proinflammatory cytokines by T lymphocytes by inhibiting calcineurin.Tacrolimus, however, appears to be 10 to 100 times as potent as an immunosuppressive. Oral tacrolimus (FK506) is used for prevention of organ rejection in recipients of renal and hepatic transplants.

• 一般的な説明

  Immunosuppressant that blocks T-cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 Binding Protein, thereby reversing its effects on sarcoplamic reticulum Ca²⁺ release. Shown to inhibit the Ca²⁺-dependent phosphatase, Calcineurin (Cat. No. 539565), as well as Na⁺-K⁺-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of Giα-3 protein.

• 臨床応用

  A topical formulation (Protopic) has recently been approved for treatment of moderate to severe atopic dermatitis in children and adults who have not responded to other therapies. Levels of systemic absorption are low even when applied to a relatively large body surface area.

• 副作用

  Local irritant reactions (burning, stinging, erythema) are a common side effect, but these usually resolve within the first few days of treatment. The major benefit of topical tacrolimus over topical corticosteroids is that tacrolimus does not cause atrophy, striae, or telangiectasia, even with chronic use.

• 参考文献

  J.H. Joe, et al., int. J. Pharm., 395, 161 (2010), DOI: 10.1016/j.ijpharm.2010.05.023.

タクロリムス 上流と下流の製品情報

タクロリムス 生産企業

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タクロリムス スペクトルデータ(MS)

104987-11-3, タクロリムス キーワード