部份中文依鲁替尼处方资料（仅供参考） 英文名：IMBRUVICA(ibrutinib) 中文名：依鲁替尼 剂  型：胶囊、片剂 研发商：强生杨森制药 药品介绍 近日，抗癌药Imbruvica（ibrutinib）获FDA批准，用于既往接受过至少一次治疗的慢性淋巴细胞白血病（CLL）患者的治疗。Imbruvica已于2013年11月获FDA批准，用于既往接受过至少一次来那度胺或其他药物治疗的套细胞淋巴瘤（MCL）患者的治疗。这2个适应症的获批，均基于整体缓解率（ORR）数据，该药对存活或疾病相关症状改善的数据尚未建立。 Imbruvica是首个每日一次、单一制剂、口服布鲁顿酪氨酸激酶（BTK）抑制剂，由强生和Pharmacyclics公司联合开发和商业化。此前，Imbruvica治疗CLL和MCL适应症均已授予优先审查资格，并根据FDA的加速批准程序批准。同时，Imbruvica也是FDA授予突破性疗法认定并获批的首批药物之一。 审批分类： 突破性药物+优先审评+加速批准+孤儿药 IMBRUVICATM(依鲁替尼[ibrutinib])胶囊，为口服使用 IMBRUVICATM(依鲁替尼[ibrutinib])片剂，为口服使用 美国初次批准：2013 作用机制 Ibrutinib是一个BTK的小-分子抑制剂。Ibrutinib与在BTK活性位点中的半胱氨酸残基形成共价键，导致BTK酶活性的抑制。BTK是B-细胞抗原受体(BCR)和细胞因子受体通路的信号分子。BTK的作用是通过B-细胞表面受体信号导致对B-细胞交易，趋化，和黏附所需通路的激活。非临床研究显示ibrutinib抑制恶性B-细胞增殖和在体内生存以及在体外细胞迁移和底物黏附。 适应证和用途 IMBRUVICA是一个激酶抑制剂适用为的治疗曾接受至少1次既往治疗有套细胞淋巴瘤(MCL)患者。 这个适应证是根据总缓解率。尚未确定生存或疾病相关症状改善. 剂量和给药方法 560 mg口服每天1次(4粒140mg胶囊每天1次)。 应用一杯水口服胶囊/片。 不要打开，破裂，或咀嚼胶囊/片. 剂型和规格 胶囊：70mg,140mg 片剂：140mg, 280mg, 420mg, 560mg 禁忌证 无。 警告和注意事项 （1）出血：对出血监视。 （2）感染：监视对发热和感染患者和及时评价。 （3）骨髓抑制：每月检查全血细胞计数. （4）肾毒性：监视肾功能和保持水化. （5）第二个原发恶性肿瘤：患者中曾发生其他恶性肿瘤，包括皮肤癌，和其他癌. （6）胚胎-胎儿毒性：可致胎儿危害。忠告妇女对胎儿潜在风险当妊娠时避免服药. 不良反应 最常见不良反应(≥20%)in患者with MCL were血小板减少，腹泻，中性粒细胞减少，贫血，疲乏，肌肉骨骼痛，外周性水肿，上呼吸道感染，恶心，瘀伤，呼吸困难，便秘，皮疹，腹痛，呕吐和食欲减低. 药物相互作用 CYP3A抑制剂：避免与强和中度CYP3A抑制剂共同给药。如中度CYP3A抑制剂必须使用，减低IMBRUVICA剂量. CYP3A诱导剂：避免与强CYP3A诱导剂共同给药. 特殊人群中使用 肝受损：在有基线肝受损患者中避免使用IMBRUVICA. 特别提示：依鲁替尼胶囊和片完整资料[附件]供患者或科研单位阅读： https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0dfd0279-ff17-4ea9-89be-9803c71bab44 IMBRUVICA ® (ibrutinib) capsules, for oral use IMBRUVICA ® (ibrutinib) tablets, for oral use Initial U.S. Approval: 2013 RECENT MAJOR CHANGES Indications and Usage:08/2017 Dosage and Administration:02/2018 Warnings and Precautions:12/2017 Mechanism of Action Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro. INDICATIONS AND USAGE IMBRUVICA is a kinase inhibitor indicated for the treatment of adult patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy. Accelerated approval was granted for this indication based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL). Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion. Waldenström's macroglobulinemia (WM). Marginal zone lymphoma (MZL) who require systemic therapy and have received at least one prior anti-CD20-based therapy. Accelerated approval was granted for this indication based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Chronic graft versus host disease (cGVHD) after failure of one or more lines of systemic therapy. DOSAGE AND ADMINISTRATION MCL and MZL: 560 mg taken orally once daily. CLL/SLL, WM, and cGVHD: 420 mg taken orally once daily. Dose should be taken orally with a glass of water. Do not open, break, or chew the capsules. Do not cut, crush, or chew the tablets. DOSAGE FORMS AND STRENGTHS Capsules: 70mg and 140mg. Tablets: 140mg, 280mg, 420mg, and 560mg. CONTRAINDICATIONS None WARNINGS AND PRECAUTIONS Hemorrhage: Monitor for bleeding and manage. Infections: Monitor patients for fever and infections, eva luate promptly, and treat. Cytopenias: Check complete blood counts monthly. Cardiac arrhythmias: Monitor for symptoms of arrhythmias and manage. Hypertension: Monitor blood pressure and treat. Second Primary Malignancies: Other malignancies have occurred in patients, including skin cancers, and other carcinomas. Tumor Lysis Syndrome (TLS): Assess baseline risk and take precautions. Monitor and treat for TLS. Embryo-Fetal Toxicity: Can cause fetal harm. Advise women of the potential risk to a fetus and to avoid pregnancy while taking the drug and for 1 month after cessation of therapy. Advise men to avoid fathering a child during the same time period. ADVERSE REACTIONS The most common adverse reactions (≥20%) in patients with B-cell malignancies (MCL, CLL/SLL, WM and MZL) were neutropenia, thrombocytopenia, diarrhea, anemia, musculoskeletal pain, rash, nausea, bruising, fatigue, hemorrhage, and pyrexia. The most common adverse reactions (≥20%) in patients with cGVHD were fatigue, bruising, diarrhea, thrombocytopenia, muscle spasms, stomatitis, nausea, hemorrhage, anemia, and pneumonia. To report SUSPECTED ADVERSE REACTIONS, contact Pharmacyclics at 1-877-877-3536 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. DRUG INTERACTIONS CYP3A Inhibitors: Dose adjustments may be recommended. CYP3A Inducers: Avoid coadministration with strong CYP3A inducers. USE IN SPECIFIC POPULATIONS Hepatic Impairment (based on Child-Pugh criteria): Avoid use of IMBRUVICA in patients with severe baseline hepatic impairment. In patients with mild or moderate impairment, reduce IMBRUVICA dose. HOW SUPPLIED/STORAGE AND HANDLING The 70 mg capsules are supplied as yellow opaque capsules, marked with "ibr 70 mg" in black ink, and are available in white HDPE bottles with a child-resistant closure: 28 capsules per bottle: NDC 57962-070-28 The 140 mg capsules are supplied as white opaque capsules, marked with "ibr 140 mg" in black ink, and are available in white HDPE bottles with a child-resistant closure: 90 capsules per bottle: NDC 57962-140-09 120 capsules per bottle: NDC 57962-140-12 Store bottles at room temperature 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F to 86°F). Retain in original package until dispensing. The IMBRUVICA (ibrutinib) tablets are supplied in 4 strengths in the following packaging configurations: 140 mg tablets: Yellow green to green round tablets debossed with "ibr" on one side and "140" on the other side. Carton of one folded blister card containing two 14-count blister strips for a total of 28 tablets: NDC 57962-014-28 280 mg tablets: Purple oblong tablets debossed with "ibr" on one side and "280" on the other side. Carton of one folded blister card containing two 14-count blister strips for a total of 28 tablets: NDC 57962-280-28 420 mg tablets: Yellow green to green oblong tablets debossed with "ibr" on one side and "420" on the other side. Carton of one folded blister card containing two 14-count blister strips for a total of 28 tablets: NDC 57962-420-28 560 mg tablets: Yellow to orange oblong tablets debossed with "ibr" on one side and "560" on the other side. Carton of one folded blister card containing two 14-count blister strips for a total of 28 tablets: NDC 57962-560-28 Store tablets in original packaging at room temperature 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F to 86°F). ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 140mg/tablets 28capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica片 140毫克/片 28片/瓶 中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 280mg/tablets 28capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica片 280毫克/片 28片/瓶 中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 420mg/tablets 28capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica片 420毫克/片 28片/瓶 中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 560mg/tablets 28capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica片 560毫克/片 28片/瓶 中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 70mg/capsules 28capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica胶囊 70毫克/粒 28粒/瓶  中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 140mg/capsules 90capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica胶囊 140毫克/粒 90粒/瓶  中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag ------------------------------------------------------- 产地国家：美国  原产地英文商品名: Imbruvica 140mg/capsules 120capsules/bottles 原产地英文药品名: ibrutinib 中文参考商品译名: Imbruvica胶囊 140毫克/粒 120粒/瓶  中文参考药品译名: 依鲁替尼 生产厂家英文名: Janssen-Cilag