英文药名: Velcade(Bortezomib Injection) 中文药名: 万珂（硼替佐米注射液） 生产厂家: ICS/MILLENNIUM 药品介绍 硼替佐米作为全球第一个靶向型抑制肿瘤细胞的蛋白酶体药物，已被87个国家用于多发性骨髓瘤的治疗，并于2008年6月被美国FDA批准作为多发性骨髓瘤的一线治疗用药。 2008年由美国、德国、英国的35家中心联合开展的Ⅱ期临床试验显示，硼替佐米单药治疗复发或难治性MCL，起效快(中位第一次缓解时间为2个疗程)，缓解时间长（中位患者可延长13.5个月的生存期），对难治性和既往2次化疗无效的患者也有效。因此，FDA批准它作为MCL治疗的二线药物。 VELCADE（硼替佐米 bortezomib）注射，粉末，冻干，用于静脉使用的溶液 初始美国批准：2003 近期主要变化 肾损伤患者 10/2007 适应症和用法，多发性骨髓瘤  06/2008 作用机制 硼替佐米是哺乳动物细胞中26S蛋白酶体的胰凝乳蛋白酶样活性的可逆抑制剂。 26S蛋白酶体是降解泛素化蛋白的大蛋白复合物。 泛素 - 蛋白酶体途径在调节特定蛋白质的细胞内浓度中起重要作用，从而维持细胞内的内环境稳定。 抑制26S蛋白酶体阻止这种靶向蛋白水解，其可以影响细胞内的多个信号级联。 这种正常稳态机制的破坏可导致细胞死亡。 实验证明，硼替佐米在体外对多种癌细胞类型具有细胞毒性。 硼替佐米在非临床肿瘤模型（包括多发性骨髓瘤）中导致体内肿瘤生长的延迟。 适应症和用法 VELCADE是一种蛋白酶体抑制剂，适用于： 治疗多发性骨髓瘤患者 治疗已接受至少1次先前治疗的套细胞淋巴瘤患者 剂量和给药 VELCADE的推荐剂量为以3至5秒推注静脉内注射施用的1.3mg/m2。 剂量调整可以用于管理在治疗期间发生的不良事件 剂量形式和强度 1单次使用的小瓶含有3.5mg硼替佐米。剂量必须个体化以防止过量。 禁忌症 VELCADE禁忌在对硼替佐米，硼或甘露醇过敏的患者中。 警告和注意事项 妇女应避免在接受VELCADE治疗时怀孕。孕妇应该知道对胎儿的潜在危害。 外周神经病变，包括严重的病例，可能发生 - 通过剂量调整或中止治疗。预先存在的严重神经病变的患者应该在经过仔细的风险 - 利益评估后用VELCADE治疗。可能发生低血压。在治疗接受抗高血压药，有晕厥病史和脱水患者时应谨慎。应密切监测具有或存在心脏病的风险因素的患者。已经报道了急性弥漫性浸润性肺疾病。 恶心，腹泻，便秘和呕吐已经发生，可能需要使用止吐和止泻药物或液体置换。 可能发生血小板减少或中性粒细胞减少;在治疗期间应定期监测全身血细胞计数。 肿瘤溶解综合征可逆后脑白质病综合征和急性肝衰竭已有报道。 不良反应 在临床研究中最常见的不良反应（发生率≥30％）包括无力状态，腹泻，恶心，便秘，周围神经病，呕吐，发热，血小板减少，精神病，厌食和食欲减退，中性粒细胞减少，神经痛，白细胞减少和贫血。已经报道了其他不良反应，包括严重的不良反应。 在特定人群中使用 建议妇女在接受VELCADE治疗时不要哺乳或怀孕。 糖尿病患者可能需要密切监测血糖和调整抗糖尿病药物。 完整处方资料附件：https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=9628 INDICATIONS AND IMPORTANT SAFETY INFORMATION FOR VELCADE® (bortezomib)INDICATIONS: VELCADE (bortezomib) is indicated for the treatment of patients with multiple myeloma and patients with mantle cell lymphoma. CONTRAINDICATIONS: VELCADE is contraindicated in patients with hypersensitivity (not including local reactions) to bortezomib, boron, or mannitol, including anaphylactic reactions. VELCADE is contraindicated for intrathecal administration. Fatal events have occurred with intrathecal administration of VELCADE. WARNINGS AND PRECAUTIONS: VELCADE(bortezomib) is for subcutaneous or IV administration only. Because each route of administration has a different reconstituted concentration, caution should be used when calculating the volume to be administered. Peripheral neuropathy, including severe cases, may occur. Patients should be monitored for symptoms and managed with dose modification or discontinuation. Patients with preexisting symptoms may experience worsening peripheral neuropathy (including ≥Grade 3). Starting with VELCADE subcutaneously may be considered for patients who either have preexisting or are at high risk for peripheral neuropathy. bullet;Hypotension: Caution should be used when treating patients receiving antihypertensives, those with a history of syncope, and those who are dehydrated. Cardiac toxicity, including acute development or exacerbation of congestive heart failure and new onset of decreased left ventricular ejection fraction, has occurred. Isolated cases of QT-interval prolongation have been reported. Patients with risk factors for, or existing, heart disease should be closely monitored. Pulmonary toxicity: Acute respiratory distress syndrome (ARDS) and acute diffuse infiltrative pulmonary disease of unknown etiology have occurred (sometimes fatal). Pulmonary hypertension, in the absence of left heart failure or significant pulmonary disease, has been reported. In the event of new or worsening cardiopulmonary symptoms, consider interrupting VELCADE until a prompt and comprehensive diagnostic evaluation is conducted. Posterior reversible encephalopathy syndrome has occurred. Consider MRI imaging for onset of visual or neurological symptoms; discontinue VELCADE if suspected. Gastrointestinal toxicity, including nausea, diarrhea, constipation, and vomiting, has occurred and may require use of antiemetic and antidiarrheal medications or fluid replacement. Interrupt VELCADE(bortezomib) for severe symptoms. Thrombocytopenia/Neutropenia: Manage with dose and/or schedule modifications. Complete blood counts should be monitored frequently during treatment. There have been reports of gastrointestinal and intracerebral hemorrhage. Support with transfusions and supportive care, according to published guidelines. Tumor lysis syndrome: Closely monitor patients with high tumor burden and take appropriate precautions. Hepatic toxicity: Monitor hepatic enzymes during treatment. Upon occurrence, interrupt therapy with VELCADE to assess reversibility. Embryo-fetal risk: Women should avoid breast-feeding or becoming pregnant while on VELCADE. Patients with diabetes may require close monitoring and adjustment of the antidiabetic medications. DRUG INTERACTIONS: Closely monitor patients receiving VELCADE (bortezomib) in combination with strong CYP3A4 inhibitors. Avoid concomitant use of strong CYP3A4 inducers. ADVERSE REACTIONS Previously untreated multiple myeloma (MM): In the phase 3 study of VELCADE administered intravenously with melphalan and prednisone (MP) vs MP alone, the most commonly reported adverse reactions (ARs) were thrombocytopenia (48% vs 42%), neutropenia (47% vs 42%), peripheral neuropathy (46% vs 1%), nausea(39% vs 21%), diarrhea (35% vs 6%), neuralgia (34% vs <1%), anemia (32% vs 46%), and leukopenia (32% vs 28%). Relapsed MM subcutaneous vs IV: In the phase 3 study of VELCADE (bortezomib) administered subcutaneously vs intravenously in relapsed MM, safety data were similar between the two treatment groups. The most commonly reported ARs in the subcutaneous vs IV treatment groups were peripheral neuropathy (37% vs 50%) and thrombocytopenia (30% vs 34%). The incidence of serious ARs was similar in the subcutaneous treatment group (20%) and the IV treatment group (19%). The most commonly reported serious ARs were pneumonia and pyrexia (each 2%) in the subcutaneous treatment group and pneumonia, diarrhea, and peripheral sensory neuropathy (each 3%) in the IV treatment group. Previously untreated mantle cell lymphoma (MCL): In a phase 3 study of VELCADE administered intravenously with rituximab, cyclophosphamide, doxorubicin, and prednisone (VR-CAP) vs vincristine, rituximab, cyclophosphamide, doxorubicin, and prednisone (R-CHOP), the most commonly reported ARs were neutropenia (87% vs 71%), thrombocytopenia (72% vs 17%), leukopenia (48% vs 36%), anemia ------------------------------------------------------------------ 产地国家: 美国 原产地英文商品名: VELCADE 3.5MG 10ML SDV PWD DPSH 1/EA 原产地英文药品名: BORTEZOMIB 中文参考商品译名: VELCADE注射粉剂 3.5毫克 10毫升/瓶 中文参考药品译名: 注射用硼替佐米 生产厂家中文参考译名: MILLENNIUM PHARMACEUTICALS 生产厂家英文名: MILLENNIUM PHARMACEUTICALS ------------------------------------------------------------------ 产地国家: 美国 原产地英文商品名: VELCADE VIAL 3.5MG D/SHIP 10ML 原产地英文药品名: BORTEZOMIB 中文参考商品译名: VELCADE注射粉剂 3.5毫克 10毫升/瓶 中文参考药品译名: 注射用硼替佐米 生产厂家中文参考译名: ICS/MILLENNIUM DIRECT 生产厂家英文名: ICS/MILLENNIUM DIRECT