英文药名：KYPROLIS（carfilzomib for Injection）

中文药名：卡非佐米冻干粉注射剂

生产厂家：小野制药

カイプロリス点滴静注用10mg／カイプロリス点滴静注用40mg

治疗类别名称
─抗肿瘤药─
蛋白酶体抑制剂
批准上市日期：2016年8月
商標名
KYPROLIS
一般名
カルフィルゾミブ（Carfilzomib）
化学名
N-｛（2S）-2-［（Morpholin-4-ylacetyl）amino］-4-phenyl-butanoyl｝-L-leucyl-L-phenylalanin-N-｛（2S）-4-methyl-1-［（2R）-2-methyloxiran-2-yl］-1-oxopentan-2-yl｝amide
構造式

分子式
C40H57N5O7
分子量
719.91
性状
该产品是一种白色至灰白色固体，N-甲基-2-吡咯烷酮，N，N-二甲基甲酰胺或易溶于二甲亚砜，甲醇或乙醇（99.5）微溶，微乙腈或2-丙醇微溶，几乎不溶于水。
批准条件
1.建立药品风险管理计划的顶部，要正确实施。
2.由于试验病人在日本是非常有限的，上市后，直至有关一定数量的病例数据集成，通过实现对一切案件的使用，结果调查显示，这使得它能够及早发现这种药物的使用患者的背景资料，数据收集这种药物的安全性和有效性，采取必要的措施，正确使用此药。
药效药理
1.作用机制
Carfilzomib通过抑制蛋白酶体的胰凝乳蛋白酶样活性，诱导肿瘤细胞的凋亡，抑制肿瘤的生长。
2.抗肿瘤作用
(1) Carfilzomib在体外试验中，抑制从MM.1S和RPMI-8226细胞系人类多发性骨髓瘤的生长。另外，它抑制RPMI-8226细胞系的生长成为MM.1S和马法兰这成为地塞米松耐抗性。
(2) Carfilzomib在免疫缺陷小鼠的MM.1S细胞系皮下植入，抑制了肿瘤的生长。
适应病症
复发或难治性多发性骨髓瘤
用法与用量
（1）每周连续2天历时2至10分钟静脉给药共三周(第1，2，8，9，15，和16天)，接着12-天休息期(第17至28天)。
（2）推荐疗程1剂量是20mg/m2/day和如果耐受增加第2疗程剂量和随后疗程剂量至27 mg/m2/day。
（3）给药前和后水化患者。
（4）在所有第1疗程剂量前用地塞米松预先给药。在第一疗程剂量递增期，和如果发生或再次出现输注反应症状时。
（5）根据毒性修改给药。
包装规格
静脉滴注
10毫克为：1瓶

40毫克为：1瓶

制造和销售
小野制药有限公司
提携
AMGEN
完整使用资料附件：http://www.info.pmda.go.jp/go/pack/4291433D1026_1_01/
Kyprolis(carfilzomib 中文药名：卡非佐米注射使用)是一种抗肿瘤药物只供利用静脉使用,也是首个蛋白酶体抑制剂适用为治疗多发性骨髓瘤患者

Ono "Kaipurorisu intravenous drip infusion for the 10mg, 40mg" get the domestic manufacturing and marketing approval of
Proteasome inhibitor "Kaipurorisu (R) for Intravenous Infusion 10mg, 40mg"
Domestic manufacturing and marketing approval for relapsed or refractory multiple myeloma
Ono Pharmaceutical Co., Ltd. (Headquarters: Chuo-ku, Osaka, President: Akatsuki Sagara, hereinafter referred to as "Company"), a proteasome inhibitor "Kaipurorisu (R) for Intravenous Infusion 10mg, 40mg" (generic name: carfilzomib, below , for the "Kaipurorisu"), today, that it has acquired the domestic manufacturing and marketing approval for the treatment of relapsed or refractory multiple myeloma, will be announced.
Multiple myeloma is a blood cancer that is caused by the abnormal plasma cells in the bone marrow, the total number of patients in Japan has been about 18,000 people and reported (※). Currently, treatment for multiple myeloma There are multiple, repeatedly traveling through the remission and relapse, or any treatment method is also not uncommon even if you want to migrate to the pathology of effective and not become intractable. In addition, in the long-term treatment has been reported side effects or complications, you might want to Difficult to treatment. From these things, it has the development of new therapeutic agents is expected for multiple myeloma.
Kaipurorisu, the Company was introduced in September 2010 than the United States Onyx Pharmaceuticals Inc (now Amgen Inc. subsidiary), is a proteasome inhibitor with high selectivity. Proteasome enzyme complex present in a cell, it has the effect of decomposing poly-ubiquitinated proteins, cell proliferation, and control the differentiation and functional cell death. Kaipurorisu by inhibiting the proteasome, induces a functional cell death of myeloma cells.
Kaipurorisu is, in July 2012 in the United States, bortezomib and have a previous history of treatment at least twice, including the immunomodulatory agent, multiple myeloma showed disease progression within 60 days, during or after the treatment the last treatment period quickly approved as a single agent therapy and efficacy and effects, and for combination therapy with lenalidomide and dexamethasone in July 2015, the approval of the multiple myeloma with the previous treatment history of one to three times as the efficacy and effect we acquired additional. In addition, in monotherapy in January 2016, it has obtained the full approval multiple myeloma with the previous treatment history of one or more times as the efficacy and effect. In Europe, in combination therapy with lenalidomide and dexamethasone in November 2015, it has been approved multiple myeloma with a previous history of treatment at least once as the efficacy and effect
It should be noted that, in Japan, on August 20, 2015, the Ministry of Health, Labour and Welfare, has been designated as orphan drug as efficacy and effect, which is scheduled for "relapsed or refractory multiple myeloma."
The Company, Kaipurorisu proper and effective in the more clinical data to be used accumulated we believe it is important. In accordance with the conditions of approval of this drug, conducted use results survey of post-marketing approval (full example research), to collect clinical data on the safety and efficacy, we will take necessary measures in the proper use of this drug .