英文药名：ICLUSIG tablets(Ponatinib Hydrochloride)

中文药名：盐酸普纳替尼片

生产厂家：大冢制药

アイクルシグ錠15mg

治疗类别名称
抗肿瘤药/酪氨酸激酶抑制剂
商標名
ICLUSIG tablets 15mg
一般名
ポナチニブ塩酸塩〔Ponatinib Hydrochloride（JAN）〕
化学名
3-［2-（Imidazo［1,2-b］pyridazin-3-yl）ethynyl］-4-methyl-N-｛4-［（4-methylpiperazin-1-yl）methyl］-3-（trifluoromethyl）phenyl｝benzamide monohydrochloride
構造式

分子式
C29H27F3N6O・HCl
分子量
569.02
性　状
包括在白色至黄色粉末有个肿块。微溶于二甲基亚砜，乙醇和微溶于水。
条件批准
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
Ponachinibu在体外，抑制ABL的酪氨酸激酶活性，包括其变体如T315I。
2.抗肿瘤作用
(1) 体外试验
Ponachinibu是，所述BCR-ABL人慢性髓性白血病衍生表达，KY01和LAMA细胞系以及小鼠表达BCR-ABL与突变诸如从Ba/F3细胞系衍生T315I原B细胞K562的增殖抑制。
(2) 体内试验
Ponachinibu是表达BCR-ABL在皮下植入小鼠K562细胞和T315I突变表明抑制肿瘤生长的Ba/F3细胞系。
适应病症
● 慢性粒细胞白血病耐药或不能耐受之前治疗的药物
● 复发或难治性费城染色体阳性的急性淋巴细胞白血病
用法与用量
成年人；每天给药一次，每次45毫克（3片）。此外，根据该状态的患者用药。
包装规格
片剂
15毫克：[塑料瓶]14片

制造厂商
大冢制药有限公司
完整治疗资料附件：http://www.info.pmda.go.jp/go/pack/4291048F1020_1_02/
ICLUSIG Tablets 15mg Approved in Japan for Patients with Chronic Myeloid Leukemia and Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia
ICLUSIG, an oral tyrosine kinase inhibitor (TKI) discovered by ARIAD Pharmaceuticals, Inc. and indicated for chronic myeloid leukemia (CML) and Philadelphia　Chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), has been approved in Japan.
ICLUSIG is already used in the U.S. and Europe for CML and Ph+ ALL patients who demonstrate resistance or intolerance to an existing TKI treatment and is awaited by patients in Asia.
Otsuka plans to market ICLUSIG in Japan, and if approved, in nine other Asian countries and regions.
Otsuka Pharmaceutical Co.Ltd. has received regulatory approval in Japan for manufacture and sales of ICLUSIG® Tablets 15 mg (ponatinib hydrochloride), a tyrosine kinase inhibitor (TKI) indicated to treat patients with chronic myeloid leukemia (CML) who are resistant or intolerant to previous treatments and patients with recurrent or refractory Philadelphia-chromosome positive acute lymphoblastic leukemia (Ph+ ALL).
Although TKIs are used as a first-line treatment for CML and Ph+ ALL, mutation of BCR-ABL genes can develop during the treatment period and indicates resistance to the currently used TKI.
In addition, intolerance to the side effects of existing TKI treatments can lead to a discontinuation of treatment.
ICLUSIG, discovered in the U.S. by ARIAD Pharmaceuticals, Inc., is a TKI that targets BCR-ABL expressed in CML and Ph+ ALL. This drug is a new chemically synthesized oral TKI, and is specifically designed to inhibit mutated TK caused by a T315I mutation which induces resistance to the currently used TKI. ICLUSIG demonstrates efficacy in CML patients with resistance to or with intolerance to currently available TKIs. ICLUSIG was approved in the U.S. in 2012, in Europe in 2013, and in 2014 Otsuka obtained the rights to commercialize and develop ICLUSIG in ten Asian countries and regions.
ICLUSIG was designated as an orphan drug in Japan and a new drug application (NDA) was submitted in January 2016. NDAs have been submitted in Korea and Taiwan as well.
Early access program until reimbursement is in place
Due to the limited existing treatment options for patients in Japan, Otsuka will provide access to ICLUSIG free of charge as soon as procedures are in place from an ethical standpoint. This program will be offered at medical institutions where clinical trials of ICLUSIG were performed and which are amenable to accepting the drug access program until the product is listed on the Japan National Health Insurance (NHI) price list. Otsuka will conduct this program in accordance with the Fair Competition Code of the Ethical Drug Manufacturing Industry.
*1 Japan, Indonesia, Malaysia, China (including Hong Kong), Philippines, Singapore, Korea, Taiwan, Thailand, Vietnam
*2 Chromosome abnormality seen in CML and Ph+ ALL. Due to translocation of Chromosome 22 and Chromosome 9, genes c-ABL and BCR bind together to form an abnormal protein which causes indefinite proliferation of hematopoietic stem cells and leads to leukemia.