近日日本厚生劳动省（MHLW）已经批准Astellas公司用于抑制器官移植后发生排异反应及在骨髓移植中出现的抗宿主反应的药物他克莫司（tacrolimus，Graceptor）缓释胶囊剂在日本上市，本品为一日1次使用，规格有0．5mg、1mg和5mg3种。 Graceptor-Graceptor降低你身体的免疫系统。免疫系统可以帮助你的身体对抗感染。免疫系统也可以打或“拒绝”一个移植的器官，如肝脏或肾脏。这是因为免疫系统会将新的器官作为一个入侵者。 Graceptor与其他药物一起使用，以防止你的身体拒绝一个心脏，肝脏或肾脏移植。 Graceptor也可用于这种药物指南中未列出的目的。 药理： 抑制细胞介导的免疫反应和某些体液免疫，但确切的机制尚不清楚。 作用于特应性皮炎的作用机制。 适应症： PO and IV器官排斥的同种异体肝，肾，或心脏移植的患者预防。用于与肾上腺皮质激素联合使用。用于与硫唑嘌呤或霉酚酸酯在心脏和肾脏移植患者一起使用。 局部的 作为二线治疗的短期和不连续长期治疗的中度至重度特应性皮炎。 未标记UsesPO和IV拒绝接收的骨髓，胰腺，胰岛细胞，以及小肠移植患者的预防，治疗自身免疫性疾病（如类风湿性关节炎）;预防急性移植物抗宿主病和治疗下列造血干细胞移植;治疗克罗恩病;治疗坏疽性脓皮病的。 白癜风的治疗，皮肤红斑狼疮，面部，弯曲，和擦烂型银屑病;口腔或生殖器扁平苔癣，坏疽性脓皮病。 Graceptor属大环内酯类抗生素。它的作用是通过减少肽基脯氨酰异构酶活性通过结合到免疫亲和素FKBP-12（FK506结合蛋白）创建一个新的复合体。这抑制了T细胞信号转导和IL-2的转录。虽然此活动类似于环孢菌素的研究表明，急性排斥的发生率降低了Graceptor使用超过环孢素。 Graceptor也被证明是有效的局部治疗湿疹，尤其过敏性湿疹。它抑制炎症以类似的方式对类固醇，但不那么强大。 Graceptor的重要皮肤优点是，它可以直接使用在脸上;外用类固醇不能用在脸上，因为它们在皮肤薄的显着存在。在身体的其他部位，局部类固醇通常是更好的治疗。 排斥反应的移植肾移植口腔预防 グラセプターカプセル0.5mg／グラセプターカプセル1mg／グラセプターカプセル5mg 商標名 Graceptor Capsules 一般名 タクロリムス水和物（Tacrolimus Hydrate） 化学名 （3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS ）-5,19-Dihydroxy-3-{（1E ）-2-［（1R,3R,4R ）-4-hydroxy-3-methoxycyclohexyl］-1-methylethenyl｝-14,16-dimethoxy-4,10,12,18-tetramethyl-8-（prop-2-en-1-yl）-15,19-epoxy-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3H -pyrido［2,1-c］［1,4］oxaazacyclotricosine-1,7,20,21（4H,23H ）-tetrone monohydrate 構造式 分子式 C44H69NO12・H2O 分子量 822.03 融点 130～133℃ 分配係数 1000以上（1-オクタノール／水系） 性状 タクロリムス水和物は白色の結晶又は結晶性の粉末である。メタノール又はエタノール（99.5）に極めて溶けやすく、N,N -ジメチルホルムアミド又はエタノール（95）に溶けやすく、水にほとんど溶けない。 取扱い上の注意 注意： 本品は高防湿性の内袋により品質保持をはかっている。 包装 カプセル0.5mg：100カプセル（10カプセル×10） カプセル1mg：100カプセル（10カプセル×10） カプセル5mg：20カプセル（10カプセル×2） 製造販売 アステラス製薬株式会社 原文处方料附件：http://www.info.pmda.go.jp/go/pack/3999014N1028_1_14/ Graceptor - Graceptor lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader. Graceptor is used together with other medicines to prevent your body from rejecting a heart, liver, or kidney transplant. Graceptor may also be used for purposes not listed in this medication guide. Pharmacology: Suppresses cell-mediated immune reactions and some humoral immunity, but exact mechanism is not known. The mechanism of action in atopic dermatitis is not known. Indication: PO and IV Prophylaxis of organ rejection in patients receiving allogenic liver, kidney, or heart transplants. Used in conjunction with adrenal corticosteroids. Used in conjunction with azathioprine or mycophenolate mofetil in heart and kidney transplant patients. Topical As second-line therapy for the short-term and noncontinuous long-term treatment of moderate to severe atopic dermatitis. Unlabeled UsesPO and IV Prophylaxis of rejection for patients receiving bone marrow, pancreas, pancreatic island cell, and small bowel transplantation; treatment of autoimmune disease (ie, rheumatoid arthritis); prevention and treatment of acute graft-versus-host disease following hematopoietic stem cell transplantation; treatment of Crohn disease; treatment of pyoderma gangrenosum. Treatment of vitiligo; cutaneous lupus erythematosis; facial, flexural, and intertriginous psoriasis; oral or genital lichen planus; pyoderma gangrenosum. Graceptor is a macrolide antibiotic. It acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 transcription. Although this activity is similar to cyclosporine studies have shown that the incidence of acute rejection is reduced by Graceptor use over cyclosporine. Graceptor has also been shown to be effective in the topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of Graceptor is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically there. On other parts of the body, topical steroid are generally a better treatment. Oral Prophylaxis of rejection in kidney graft transplant --------------------------------------------------------------- Graceptor® Capsules 0.5mg, 1mg, 5mg (generic name: tacrolimus hydrate) will become available in Japan on October 28, 2008 with the indication of “suppression of organ rejection” and “suppression of graft rejection and graft versus host disease (GVHD) in bone marrow transplantation.”  Graceptor is a once-daily modified release formulation of Astellas’s Prograf® (tacrolimus, twice-daily formulation). Tacrolimus works as an immunosuppressant by inhibiting activation of T-cell. Graceptor maintains its efficacy and safety at the similar level with the existing drug, Prograf. Once-daily administration possibly contributes to reduce physical and mental stress for patients who need to take several different medications in a long-term. It is expected to improve compliance with its more convenient once-daily dosing option, and may lead to improve long term outcomes of transplantation. Once-daily formulation of Prograf has been available with the brand name Advagraf® in 19 countries worldwide including Europe. Astellas expects to provide a new option for transplant medication with the new lineup for Prograf family. Details of approval are as follows: Date of marketing approval: July 16, 2008 Brand name: Graceptor® Capsules 0.5mg, 1mg and 5 mg Generic name: tacrolimus hydrate Classification: Immunosuppressant Indication:  　Suppression of organ rejection in the following organ transplantation Kidney transplantation, liver transplantation, 　heart transplantation,lung transplantation, pancreas transplantation 　Suppression of graft rejection and graft versus host disease (GVHD) in bone　marrow transplantation Dosage and administration: [Kidney transplantation] Usually, a dose of 0.15 - 0.20 mg/kg as tacrolimus is orally administered, once daily from the morning 2 days before transplantation. The dosage may be adjusted thereafter depending on the patient’s symptoms. [Liver transplantation] Usually, in the early postoperative period, a dose of 0.10 - 0.15 mg/kg as tacrolimus, is orally administered once daily in the morning. The dosage may be adjusted thereafter depending on the patient's symptoms. [In case of converting from oral Prograf to this product (in kidney transplantation, liver transplantation, heart transplantation, lung transplantation, pancreas transplantation, or bone marrow transplantation)] In case of converting from oral Prograf to this product, the usual dosage for oral use is the same as the daily dose of oral Prograf, once daily in the morning. Approval holder:  Astellas Pharma Inc. ------------------------------------------------ 产地国家: 日本 原产地英文商品名: Graceptor 5mg 20 Caps 原产地英文药品名: TACROLIMUS 中文参考商品译名: Graceptor胶囊剂 5毫克 20胶囊/盒 中文参考药品译名: 他克莫司 生产厂家中文参考译名: 安斯泰来 生产厂家英文名: astellas ------------------------------------------------ 产地国家: 日本 原产地英文商品名: Graceptor 1mg 100Caps 原产地英文药品名: TACROLIMUS 中文参考商品译名: Graceptor胶囊剂 1毫克 100胶囊/盒 中文参考药品译名: 他克莫司 生产厂家中文参考译名: 安斯泰来 生产厂家英文名: astellas ------------------------------------------------ 产地国家: 日本 原产地英文商品名: Graceptor 0.5mg 100Caps 原产地英文药品名: TACROLIMUS 中文参考商品译名: Graceptor胶囊剂 0.5毫克 100胶囊/盒 中文参考药品译名: 他克莫司 生产厂家中文参考译名: 安斯泰来 生产厂家英文名: astellas