癌症罕用药物普乐沙福注射液（Mozobil）在美国FDA批准上市 美国FDA批准基Genzyme公司的plerixafor注射液（Mozobil）上市，与粒细胞集落刺激因子（G-CSF）联合用药促进红细胞生成素干细胞进入非霍奇金淋巴瘤（NHL）和多发性骨髓瘤（MM）患者血流以收集、随后自体移植。本品还被获准作为罕用药物。 本品系一新颖的小分子CXCR4趋化因子受体阻断剂，在多项早期研究显示可快速有效地增加NHL和MM患者血液循环中的干细胞数。 本品在治疗需干细胞移植的某些类型癌症患者是一重大进展。由于本品有益于患者、医生和移植治疗中心将成为干细胞移植治疗方案的整体部分。 本品调动红细胞生成素干细胞从骨髓进入血流，收集、为需干细胞移植的某些类型癌症患者进行移植。 以往，移植前患者需接受处方药化疗和（或）生长因子类药物来帮助其调动红细胞生成素干细胞进入血流。一旦此细胞进入血流，它们被收集用于移植制备。 批准日期：2009年8月  公司：健赞制药公司 Mozobil（普乐沙福 plerixafor注射）解决方案使用皮下 美国初始批准：2008 作用机理 Plerixafor是CXCR4的趋化因子受体并阻断其同源配体，基质细胞衍生因子1α（SDF-1α）的结合的抑制剂。 SDF-1α和CXCR4被认为发挥贩运和人造血干细胞（HSC）的归巢作用是骨髓舱。一旦在骨髓，干细胞的CXCR4可起到帮助锚定这些细胞的骨髓基质，可以通过SDF-1α或通过其他粘附分子的诱导直接。与plerixafor治疗导致白细胞增多和海拔在小鼠，狗和人造血循环祖细胞。通过动员plerixafor CD34 +细胞能植入与长期再生能力长达一年犬移植模型。 适应症和用法 Mozobil，造血干细胞动员，指示结合粒细​​胞集落刺激因子（G-CSF），以动员造血干细胞的外周血收集和随后的自体移植的患者的非霍奇金淋巴瘤和多发性骨髓瘤。 用法用量 •启动治疗Mozobil患者接受的G-CSF后，每天一次，4天。 •重复Mozobil剂量最多连续4天。 •选择剂量以0.24毫克/公斤实际体重。 •通过单采开始大约11小时前，皮下注射辖。 •肾损害：如果肌酐清除率≤50 mL/min的剂量减少三分之一至0.16毫克/公斤。 剂型和规格 •含有20毫克/毫升溶液1.2毫升一次性使用小瓶中。 禁忌 •无。 警告和注意事项 白血病患者肿瘤细胞动员：Mozobil小动员白血病细胞，不应该在白血病患者中使用。 血液系统的影响：增加循环中的白细胞和血小板数量减少已被观察到。监控Mozobil在使用过程中的血细胞计数和血小板计数。 对肿瘤细胞动员潜力：肿瘤细胞从四月骨髓造血干细胞动员Mozobil和G-CSF时被释放。肿瘤细胞回输的效果是未知的。 潜在脾破裂：评估谁报告说左上腹和/或肩胛或肩部疼痛的患者。 妊娠：可能引起胎儿危害。提醒女性没有服用Mozobil时怀孕。 不良反应 最常见的不良反应（≥10％）：腹泻，恶心，疲劳，注射部位反应，头痛，关节痛，头晕和呕吐。 Mobilizing hematopoietic stem cells to bloodstream  COMPANY: Genzyme PHARMACOLOGIC CLASS: Hematopoietic stem ACTIVE INGREDIENT: Plerixafor 20mg/mL; soln for SC inj; preservative-free INDICATION: In combination with granulocyte colony stimulating factor (G-CSF): To mobilize hematopoietic stem cells to the peripheral blood for collection and autologous transplantation in patients with non-Hodgkin's lymphoma or multiple myeloma. PHARMACOLOGY: Patient with non-Hodgkin's lymphoma or multiple myeloma may be candidates for autologous hematopoietic stem cell transplantation as part of their treatment. Before the transplant can take place, a minimum number of stem cells, generally about 2 million/kg, must be collected. For some patients, this may be a lengthy process or may not occur satisfactorily at all. Plerixafor is a CXCR4 chemokine receptor antagonist that is designed to mobilize hematopoietic stem cells from the bone marrow to the bloodstream where they can be harvested, enabling certain patients to proceed to transplant. It blocks the binding of stromal cell-derived factor-1a, which, with CXCR4, plays a role in the homing and trafficking of stem cells in the bone marrow. Treatment with plerixafor causes increases in circulating leukocytes and stem cells. CLINICAL TRIALS: Two placebo-controlled studies were conducted to evaluate the safety and efficacy of plerixafor in combination with G-CSF for stem cell mobilization. In the first study, conducted in patients with non-Hodgkin's lymphoma, 59% of 150 patients given plerixafor + G-CSF collected >5 x 106 CD34+ cells/kg in four or fewer apheresis sessions, compared to 20% of 148 patients given placebo + G-CSF. In the second study, conducted in patients with multiple myeloma, 72% of 148 patients who were treated with plerixafor + G-CSF collected >6 x 106 CD34+ cells/kg from the peripheral blood in two or fewer apheresis sessions, compared with 34% of 154 patients given placebo + G-CSF. The target numbers of stem cells in the studies were chosen based on literature that suggests that reaching these targets can help to facilitate engraftment. Updated 12-month follow-up findings showed that graft durability rates for patients in the plerixafor + G-CSF and placebo + G-CSF arms were comparable. ADULTS: Start after 4 days' treatment with G-CSF. Give approximately 11 hours before starting apheresis. Repeat up to 4 consecutive days. Base dose on actual body weight. 0.24mg/kg SC; max 40mg/day. Renal impairment (CrCl≤50mL/min): 0.16mg/kg; max 27mg/day. CHILDREN: Not recommended. PRECAUTIONS: Not for use in leukemia. May cause mobilization of tumor cells. Monitor blood and platelet counts (esp. neutrophils). Monitor for splenic rupture (eg, left upper quadrant/scapular or shoulder pain). Pregnancy (Cat.D); avoid. Nursing mothers: not recommended. INTERACTIONS: May be potentiated by drugs that reduce renal function or compete for active tubular secretion. ADVERSE REACTIONS: GI upset, fatigue, injection site reactions, headache, arthralgia, dizziness; tumor cell mobilization, increased circulating neutrophils, decreased platelet counts, enlarged spleen, vasovagal reaction may occur. HOW SUPPLIED: Single-use vials (1.2mL)—1 Important Safety Information •Mozobil is not intended for HSCT mobilization and collection in patients with leukemia. •Mozobil in combination with G-CSF increases circulating WBCs. Your WBC counts will be monitored. •Thrombocytopenia (a decrease in the number of platelets circulating in the blood) has been observed in patients receiving Mozobil. Your platelet counts will be monitored. •Cancer cells may be released from the bone marrow and subsequently collected along with your stem cells during apheresis. The potential effects of infusing cancer cells during your transplant have not been well-studied. •Your spleen may be examined if you experience pain in the left upper stomach area or left shoulder area as these may be signs of an enlarged or burst (ruptured) spleen. •Mozobil may harm the unborn child when administered to a pregnant woman. Scientific studies have shown that Mozobil caused harm to unborn animals. The safety of Mozobil in pregnant women has not been established in clinical trials. If you are of childbearing potential you should be advised to avoid becoming pregnant while receiving treatment with Mozobil. If this drug is used during pregnancy, or if you become pregnant while taking this drug, you should be apprised of the potential hazard to the unborn child. •The most common adverse reactions (occurring in greater than or equal to 10% of patients) during HSC mobilization and apheresis were: diarrhea (37%), nausea (34%), tiredness (fatigue) (27%), injection site reaction (34%), headache (22%), pain in your joints (arthralgia) (13%), dizziness (11%), and vomiting (10%). https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a56b1b78-0ae2-41b4-9c76-98ad9d439199 ------------------------------------------------------- 产地国家：美国  原产地英文药品名： PLERIXAFOR 中文参考药品译名： 普乐沙福 原产地英文商品名： MOZOBIL 20mg/ml 1.2ml/vial 中文参考商品译名： MOZOBIL 20毫克/毫升 1.2毫升/瓶 生产厂家英文名： GENZYME 生产厂家中文参考译名： 健赞