部份中文来那度胺资料（仅供参考） 来那度胺（lenalidomide），主要用于治疗慢性骨髓瘤和有5q缺失的骨髓增生异常综合症(Myelodysplastic syndrome, MDS)。来那度胺是沙利度胺的新一代衍生物，但没有发现其具有致畸变的毒性，并且药效比沙利度胺强100倍。根据三期临床试验的结果，来那度胺是目前治疗多发性骨髓瘤疗效最显著的药品，超过一半的病人服用该药后可以延长存活时间达到3年以上。 Revlimid它也是唯一可以治疗骨髓增生异常综合症（MDS）的药物，临床结果发现64％的MDS病人用来那度胺治疗后无需再用输血来治疗MDS。 通用名：来那度胺 英文名称：lenalidomide 成份：来那度胺 规格： 5、10、15、20mg 适应症： 用于治疗骨髓增生异常综合征。 用法用量： 推荐初始剂量为25mg/天，1-20天；40mg/天，21-28天；可根据临床化验结果进行适当的调节。 敬告患者：因抗肿瘤药品比较特殊，建议患者购买任何抗癌药品须由专业肿瘤科医生处方后取药，医嘱用药，才能安全、有效。 REVLIMID - lenalidomide capsule  Celgene Corporation REVLIMID® (lenalidomide) in combination with dexamethasone is indicated for the treatment of multiple myeloma (MM) patients who have received at least one prior therapy. REVLIMID® (lenalidomide) is indicated for patients with transfusion-dependent anemia due to Low- or Intermediate-1–risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities. Important Safety Information CONTRAINDICATIONS: Pregnancy Category X: •Lenalidomide is contraindicated in pregnant women and women capable of becoming pregnant. Females of childbearing potential may be treated with lenalidomide provided adequate precautions are taken to avoid pregnancy Allergic Reactions: •REVLIMID is contraindicated in patients who have demonstrated hypersensitivity (e.g., angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis) to lenalidomide WARNINGS AND PRECAUTIONS: Fetal Risk: •REVLIMID is an analogue of thalidomide, a known human teratogen that causes life-threatening human birth defects. An embryofetal development study in non-human primates indicates that lenalidomide produced malformations in the offspring of female monkeys who received the drug during pregnancy, similar to birth defects observed in humans following exposure to thalidomide during pregnancy. If REVLIMID is used during pregnancy, it may cause birth defects or death to a developing baby •Females of childbearing potential must be advised to avoid pregnancy while on REVLIMID. Two effective contraceptive methods should be used during therapy, during therapy interruptions, and for at least 4 weeks after completing therapy •Male Patients: It is not known whether lenalidomide is present in the semen of patients receiving the drug. Therefore, males receiving REVLIMID must always use a latex condom during any sexual contact with females of childbearing potential, even if they have undergone a successful vasectomy Reproductive Risk and Special Prescribing Requirements (RevAssist® Program): •Because of this potential toxicity and to avoid fetal exposure, REVLIMID is only available under a special restricted distribution program called "RevAssist." Prescribers and pharmacists registered with the program can prescribe and dispense the product to patients who are registered and meet all the conditions of the RevAssist® program Hematologic Toxicity—Multiple Myeloma: •REVLIMID can cause significant neutropenia and thrombocytopenia •Patients taking REVLIMID for MM should have their complete blood counts monitored every 2 weeks for the first 12 weeks and then monthly thereafter •In the pooled MM studies Grade 3 and 4 hematologic toxicities were more frequent in patients treated with the combination of REVLIMID and dexamethasone than in patients treated with dexamethasone alone •Patients may require dose interruption and/or dose reduction Deep Vein Thrombosis: •Venous thromboembolic events (predominantly deep venous thrombosis and pulmonary embolism) have occurred in patients with MM treated with lenalidomide combination therapy and patients with MDS treated with lenalidomide monotherapy Allergic Reactions: •Angioedema and serious dermatologic reactions including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) have been reported. These events can be fatal. Patients with a prior history of Grade 4 rash associated with thalidomide treatment should not receive REVLIMID. REVLIMID interruption or discontinuation should be considered for Grade 2-3 skin rash. REVLIMID must be discontinued for angioedema, Grade 4 rash, exfoliative or bullous rash, or if SJS or TEN is suspected, and should not be resumed following discontinuation for these reactions Tumor Lysis Syndrome: •Fatal instances of tumor lysis syndrome have been reported during treatment with lenalidomide. The patients at risk of tumor lysis syndrome are those with high tumor burden prior to treatment. These patients should be monitored closely and appropriate precautions taken Tumor Flare Reaction: •Tumor flare reaction has occurred during investigational use of lenalidomide for chronic lymphocytic leukemia (CLL) and lymphoma, and is characterized by tender lymph node swelling, low grade fever, pain and rash. Treatment of CLL or lymphoma with lenalidomide outside of a well-monitored clinical trial is discouraged DRUG INTERACTIONS: •Erythropoietic agents, or other agents, that may increase the risk of thrombosis, such as estrogen containing therapies, should be used with caution in MM patients receiving lenalidomide with dexamethasone USE IN SPECIAL POPULATIONS: Nursing Mothers: •It is not known whether REVLIMID is excreted in human milk •Because of the potential for adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother Geriatric Use: •Since elderly patients are more likely to have decreased renal function, care should be taken in dose selection. Monitor renal function Renal Impairment: •Since REVLIMID is primarily excreted unchanged by the kidney, adjustments to the starting dose of REVLIMID are recommended to provide appropriate drug exposure in patients with moderate or severe renal impairment (CLcr < 60 mL/min) and in patients on dialysis ADVERSE REACTIONS: Multiple Myeloma •In the REVLIMID/dexamethasone treatment group, 269 patients (76%) underwent at least one dose interruption with or without a dose reduction of REVLIMID compared to 199 patients (57%) in the placebo/dexamethasone treatment group •Of these patients who had one dose interruption with or without a dose reduction, 50% in the REVLIMID/dexamethasone treatment group underwent at least one additional dose interruption with or without a dose reduction compared to 21% in the placebo/dexamethasone treatment group •Most adverse events and Grade 3/4 adverse events were more frequent in MM patients who received the combination of REVLIMID/dexamethasone compared to placebo/dexamethasone •Adverse reactions reported in ≥15% of MM patients (REVLIMID/dexamethasone vs dexamethasone/placebo): fatigue (44% vs 42%), neutropenia (42% vs 6%), constipation (41% vs 21%), diarrhea (39% vs 27%), muscle cramp (33% vs 21%), anemia (31% vs 24%), pyrexia (28% vs 23%), peripheral edema (26% vs 21%), nausea (26% vs 21%), back pain (26% vs 19%), upper respiratory tract infection (25% vs 16%), dyspnea (24% vs 17%), dizziness (23% vs 17%), thrombocytopenia (22% vs 11%), rash (21% vs 9%), tremor (21% vs 7%), weight decreased (20% vs 15%), nasopharyngitis (18% vs 9%), blurred vision (17% vs 11%), anorexia (16% vs 10%), and dysgeusia (15% vs 10%) Myelodysplastic Syndromes •Thrombocytopenia (61.5%; 91/148) and neutropenia (58.8%; 87/148) were the most frequently reported adverse events observed in the del 5q MDS population •Other adverse events reported in ≥15% of del 5q MDS patients (REVLIMID): diarrhea (49%), pruritus (42%), rash (36%), fatigue (31%), constipation (24%), nausea (24%), nasopharyngitis (23%), arthralgia (22%), pyrexia (21%), back pain (21%), peripheral edema (20%), cough (20%), dizziness (20%), headache (20%), muscle cramp (18%), dyspnea (17%), pharyngitis (16%), epistaxis (15%), asthenia (15%), upper respiratory tract infection (15%) DOSAGE AND ADMINISTRATION: •Treatment is continued or modified based upon clinical and laboratory findings. Dosing modifications are recommended to manage Grade 3 or 4 neutropenia or thrombocytopenia or other Grade 3 or 4 toxicity judged to be related to REVLIMID •For other Grade 3 or 4 toxicities judged to be related to REVLIMID, hold treatment and restart at next lower dose level when toxicity has resolved to ≤Grade 2 Please see full Prescribing Information, including Boxed WARNINGS, CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS, and ADVERSE REACTIONS. REVLIMID®, RevAssist®, RevAssist® Online, and Celgene Patient Support® are registered trademarks of Celgene Corporation. FDA已批准药物来那度胺(通用名：lenalidomide)用于治疗患亚型骨髓增生异常综合症（Myelodysplastic Syndrome，MDS）的病人。该亚型是5q缺失染色体异常（deletion 5q cytogenetic abnormality）的MDS病人。 MDS是一种异常的集合，包括骨髓不能正常发挥功能，并且身体不能制造足够的正常血细胞。患MDS的病人可能需要血液和血小板输注及抗生素疗法以抗感染。在临床试验中，接受来那度胺治疗的病人不再需要输血，多数病人3个月内不需要输血。输血免除期平均持续44星期。 “该新产品将为遭受这种罕见病的病人提供非常需要的治疗选择，在一些病例中，这种罕见病被发现已发展成致命型白血病。”FDA的CDER主任Steven Galson医学博士称。 MDS可以在其他疾病的药物疗法或放射疗法后生成，或者在无已知起因的情况下生成。一些类型的MDS可以发展成急性骨髓白血病（AML），一种生成太多白细胞的癌症类型。估计美国每年诊断出7000到12000 个MDS新病例。尽管MDS在所有年龄群发生，但在60岁以上的人群中发病率最高。典型症状包括体虚、疲劳、感染、易瘀伤、出血及发烧。来那度胺结构上类似于反应停（thalidomide），一种已知导致严重出生缺陷的药物。更多研究正在动物中进行，以解决当怀孕期间服用Revlimid是否也有导致出生缺陷的风险。尽管这些研究还在进行中，该公司正在一个称为RevAssist的旨在预防胎儿暴露的风险管理计划下销售来那度胺。 根据RevAssist，只有在该计划中登记的药剂师和处方者能处方和分发来那度胺。该计划要求病人，包括女性病人进行强制性孕期检测，以在开始服用 Revlimid前提供知情同意。医生将检查孕期测试，限制处方为一个月的邮寄供应，并将任何孕期服用报给FDA。当进一步关于出生缺陷的动物测试结果完成时，FDA和生产商将再评价该风险管理计划。来那度胺的标签将包括一个黑框警告（Black Box Warning）和一个关于胎儿暴露预防的药物指南（Medication Guide）。另外的黑框警告包括因血球计数抑制和血栓风险增加而可能需要降低剂量。常见的报道与Revlimid有关的副作用包括血小板减少（低血小板计数）、嗜中性白血球减少症（低白细胞记数）、腹泻、搔痒（痒）、皮疹和疲劳 RevAssist临床多发性骨髓瘤治疗特点 Lenalidomide是thalidomide的结构类似体，拥有类似但更强力的生物活性。针对多发性骨髓瘤具有很好的治疗作用，可以显著延长这些癌症病人的生命并提高其生活质量。它是迄今为止对针对多发性骨髓瘤疗效最好的药物。它还对5q染色体缺失的骨髓增生异常综合症也有好的治疗作用。 日前，美国食品药品管理局（FDA）批准了美国细胞基因公司的来那度胺的一个新适应证，即合用地塞米松（Dexamethasone）治疗已经接受过至少一种疗法的多发性骨髓瘤患者。 来那度胺属免疫调节剂。在临床试验中，来那度胺合用地塞米松治疗的大多数副反应和严重副反应都较单用地塞米松疗法更为频繁。 另外，因来那度胺是沙利度胺（Thalidomide）的衍生物，故其仍具有导致生育缺陷的潜在危险，临床处方必须严格遵照一项专有特殊程序办理。 来那度胺）与地塞米松联合治疗复发或顽固性多发骨髓瘤的试验中，351名已接受至少一种原抗骨髓瘤治疗的患者，随机分成为2组，一组176人在第1-21天每日口服25mg lenalidomide，对照组175人，服用安慰剂，28天为一循环。另外，所有患者在前4个循环中第1-4天，第9-12天，第17-20天，每日口服地塞米松40mg，前4循环过后，仅在第1-4天服用。如某患者出现疾病进展或不可耐受的毒性反应，即终止试验。原定试验终止点为疾病进展时间点。 结果： 服用lenalidomide及地塞米松(lenalidomide组)的患者，疾病进展时间点明显晚于服用安慰剂与地塞米松组（安慰剂组）（平均值为 11.3个月v.s.4.7个月；P<0.001）。lenalidomide组中106名患者表现为完全或部分应答（60.2%），安慰剂组42名患者（24.0%，P<0.001），完全应答率分别15.9%，3.4%（P<0.001）。lenalidomide组总体存活率明显改善（死亡危险比，0.66；P=0.03）。lenalidomide组，大于10%的患者发生3级或4级副作用，包括中性粒细胞减少(29.5%, vs. 安慰剂组2.3%)，血小板减少症(11.4% vs. 5.7%)，和静脉血栓(11.4% vs. 4.6%)。 结论： Lenalidomide联合地塞米松比单纯高剂量地塞米松治疗复发或顽固性多发骨髓瘤更有效。 推荐依据及理由 多发性骨髓瘤是一种恶性浆细胞增生性血液肿瘤。浆细胞具有分泌免疫球蛋白的功能，但是大部分多发性骨髓瘤患者增生的浆细胞只产生一种称为副蛋白（paraprotein）或M蛋白的对身体无益的免疫球蛋白，正常的浆细胞和其它白细胞被恶性浆细胞替代，导致正常免疫球蛋白合成与分泌减少。多发性骨髓瘤细胞还侵犯身体其它组织如骨组织，并导致肿瘤发生。 多发性骨髓瘤是第二大血液肿瘤，患者人数约占所有肿瘤患者的1%，死亡人数约占所有癌症死亡人数的2%。全球约有20万患者。估计2004年全球约有7.4万新发病例，2005年死亡病例可达6万人。 来那度胺是一种新的调节免疫型、非化学疗法抗癌药物，其化学成分与沙利度胺（thalidomide）相类似，但在实验应用中疗效更显着，而且没有出现服用沙利度胺所经常产生的一些副作用。 revlimid对细胞内多种生物途径都有影响。目前celgene公司仍在进行本品的血液学和肿瘤学治疗作用评估，包括多发性骨髓瘤、骨髓增生异常综合征、慢性淋巴细胞白血病以及实体瘤。骨髓增生异常综合征是一种恶性血液疾病，全球大约有30万患者。当骨髓中的血细胞始终处于不成熟阶段从而不能履行其必要功能时，骨髓增生异常综合征就会发生。骨髓中充满了这些不成熟细胞，抑制了正常细胞的发展。骨髓增生异常综合征患者必须经常依靠输血来抵抗贫血、疲劳等症状，直到发展成为威胁生命的铁超负荷或者铁中毒。该疾病的治疗迫切需要一种治本的方法而不仅仅是控制症状。超过一半的骨髓增生异常综合征患者诊断出细胞染色体变异，包括一个以上染色体的部分或完全缺失。骨髓增生异常综合征中最常见的细胞染色体异常出现在5、7和20号染色体的q缺失。另一比较普遍的变异是8号染色体的额外复制。5q染色体的缺失在骨髓增生异常综合征患者中的比例可达20％～30％。 特别提醒：21粒包装由是美国细胞基因公司（Celgene）生产，此产品规格为；5mg.10mg.15mg.25mg。目前在香港、美国、韩国、澳洲同步上市 http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=10442 http://ir.celgene.com/releasedetail.cfm?ReleaseID=821055 ----------------------------------------------------- 注：以下产品不同规和不同价格，购买时请以咨询为准！ ------------------------------------------------------ 产地国家：美国 原产地英文商品名: REVLIMID 10mgX30capsules 原产地英文药品名: LENALIDOMIDE 中文参考商品译名: 雷利米得 10毫克x30胶囊/瓶 中文参考药品译名: 雷纳利多米得 曾用名: 来那度胺 生产厂家中文参考译名: 细胞基因公司 生产厂家英文名: Celgene --------------------------------------------------------------- 产地国家：美国 原产地英文商品名: REVLIMID 5mgX30capsules 原产地英文药品名: LENALIDOMIDE 中文参考商品译名: 雷利米得 5毫克x30胶囊/瓶 中文参考药品译名: 雷纳利多米得 曾用名: 来那度胺 生产厂家中文参考译名: 细胞基因公司 生产厂家英文名: Celgene --------------------------------------------------------------- 产地国家：美国 原产地英文商品名: REVLIMID 5MGx100capsules 原产地英文药品名: LENALIDOMIDE 中文参考商品译名: 雷利米得 5毫克x100胶囊/瓶 中文参考药品译名: 雷纳利多米得 曾用名: 来那度胺 生产厂家中文参考译名: 细胞基因公司 生产厂家英文名: Celgene --------------------------------------------------------------- 产地国家：美国 原产地英文商品名: REVLIMID 10mgX100capsules 原产地英文药品名: LENALIDOMIDE 中文参考商品译名: 雷利米得 10毫克x100胶囊/瓶 中文参考药品译名: 雷纳利多米得 曾用名: 来那度胺 生产厂家中文参考译名: 细胞基因公司 生产厂家英文名: Celgene