部份中文曲贝替定处方资料（仅供参考）
英文名：Trabectedin
商品名：Yondelis I.V.
中文名：曲贝替定冻干粉注射剂
生产商：大鹏药业
药品简介
Yondelis（Trabectedin，曲贝替定）是一种全新非铂类药，由西班牙Zeltia制药公司研发生产，2007年9月被批准用来治疗晚期软组织肉瘤；现在又获得欧洲监管机构批准，用来治疗卵巢癌。
ヨンデリス点滴静注用0.25mg／ヨンデリス点滴静注用1mg
药物分类名称
抗肿瘤药
批准日期：2015年12月
商標名
Yondelis I.V. infusion 0.25mg
Yondelis I.V. infusion 1mg
構造式
一般名
トラベクテジン（Trabectedin）
化学名
（1'R,6R,6aR,7R,13S,14S,16R）-6',8,14-Trihydroxy-7',9-dimethoxy-4,10,23-trimethyl-19-oxo-3',4',6a,7,12,13,14,16-octahydro-2'H,6H-spiro[6,16-（epithiopropanooxymethano）-7,13-epiminobenzo［4,5］azocino［1,2-b］［1,3］dioxolo［4,5-h］isoquinolin-20,1'-isoquinolin]-5-yl acetate
分子式
C39H43N3O11S
分子量
761.84
融点
155～162℃（分解）
性状
它是一种白色的粉末。 它易溶于N，N-二甲基甲酰胺，甲醇，乙醇（99.5）或乙酸（100），微溶于丙酮，较不溶于二氯甲烷或乙腈，难溶于水。
批准条件
制定药品风险管理计划，适当实施。
2.由于日本的临床试验数量非常有限，通过对所有病例进行使用情况调查，直到制作和销售后累积一定数量的病例， 除了掌握使用这种药物的患者的背景信息外，尽快收集有关该药物安全性和有效性的资料，并采取必要措施，以正确使用该药物。
药效药理
1. 抗肿瘤効果
该产品是源自人滑膜肉瘤的SYO-1细胞系，源自人尤因肉瘤的SK-ES-1细胞系，源自人肺泡横纹肌肉瘤的SJCRH 30细胞系，源自人骨肉瘤的KHOS / NP细胞系 ，衍生自人横纹肌肉瘤的RD细胞系和皮下移植人源性平滑肌肉瘤SK-LMS-1细胞系的裸鼠。
2. 作用机序
该试剂与DNA的小沟结合，通过抑制核苷酸切除修复机制等引起细胞死亡和细胞周期停滞，从而抑制肿瘤生长。
此外，该药物抑制FUS-CHOP蛋白和EWS-FLI1蛋白在人粘液脂肪肉瘤和人类Ewing肉瘤中作为转录因子表达的EWS-FLI1蛋白的功能，以及癌相关基因的表达 据报道控制。
适应病症
恶性软组织肿瘤
用法及与用量
通常，以1.2mg/m 2（体表面积）的剂量静脉滴注1.2小时，每天一次，作为trabectein 24小时，然后停药至少20天。 以此作为一个周期重复管理。 此外，根据患者的状况进行体重减轻。
包装规格
静脉滴注
0.25mg：1瓶
1mg：1瓶
制造厂商
大鵬制药有限公司
完整说明书附件：http://www.info.pmda.go.jp/go/pack/4291431D1027_1_05/
New antineoplastic agent "Yondelis® for intravenous drip infusion" Manufacture and market approval for the efficacy and effect of malignant soft tissue tumor
September 28, 2015 Taiho Pharmaceutical Co., Ltd. New antineoplastic agent "Yondelis® for intravenous drip infusion" Obtained manufacturing and marketing approval based on indication of malignant soft tissue tumor
Taiho Pharmaceutical Industry Co., Ltd. (Headquarters: Tokyo, President: Masayuki Kobayashi) announced today that it has entered into an agreement with Otsuka Pharmaceutical Co., Today, we will inform you that we have obtained manufacturing and marketing approval from the Ministry of Health, Labor and Welfare due to the efficacy and effect of "Malignant Soft Tumor".
This drug is an antineoplastic agent that was created by Pharmamar, Spain. Originally isolated from Ecteinascidia turbinata (Ecteinasiaia · Turbinata), a natural product is now a synthetic method is established. Taiho Pharmaceutical has concluded a licensing agreement for development and sales in Japan with Pharmamar in 2009 and has been developing this drug.
Taiho Pharmaceutical conducted three clinical trials in Japan for this approval. First, in 2010 we started Phase I clinical trial (10045020 test) for patients with malignant soft tissue tumors for the purpose of examining the recommended dose. Afterwards, randomized Ⅱ (control group) was compared with progression-free survival time of the group treated with this drug and the supportive care (BSC: Best Supportive Care) group for patients with malignant soft tissue tumors of histological type * 1 for which chromosomal translocation was reported Phase II safety study (10045040 test) was conducted on patients who were assigned to the BSC group of the phase comparison test (10045030 test) and 10045030 test and then administered with this drug after the disease progression was confirmed and the study was discontinued Did. As a result of the 10045030 test, it was clinically useful because the administration group of this drug was more effective than the BSC group, side effects were controlable by appropriate measures such as weight reduction, drug withdrawal and symptomatic treatment It was shown. In addition, this product has been designated as a drug for rare diseases in June 2011.
Taiho Pharmaceutical expects that this drug can contribute to the treatment of patients as a new therapeutic option for malignant soft tumors with high unmet / medical needs.
About malignant soft tissue tumor
It is an intractable malignant tumor that develops in the soft tissues of the body (muscle, connective tissue, fat, blood vessel lymphatic vessels, etc.). The annual morbidity rate in Japan is about 2-3 people per 100,000 people, and it is a rare illness with estimated number of patients of about 5,000 * 2.
About Yondelis
Yondelis is a natural product (an alkaloid compound having three tetrahydroisoquinoline rings) originally isolated from a kind of sea squirt of the Caribbean sea, and now we have established a synthetic method. This drug is an antineoplastic agent that binds to DNA and shows effects on cell division, gene transcription, DNA repair mechanism, and is effective in Europe in September 2007 "Invalid for anthracycline drugs and ifosfamide, Treatment of advanced malignant soft tissue tumors of adults not suitable for administration of drugs "has been approved as an indication. In the world, it is approved in 77 countries / regions * 3 such as Europe, South America, Asia etc.
About Pharmamar
Pharmamar is a global biopharmaceutical company based in Madrid, Spain, contributing to the advancement of cancer medical care through the discovery and development of innovative anticancer drugs derived from marine products. In addition to developing a rich pipeline as a candidate for a new drug and a robust oncology research and development program, in Europe, Yondelis is developed and marketed as a therapeutic agent for advanced malignant soft tumor, recurrent platinum-sensitive ovarian cancer, solid cancer and blood Currently we are developing clinical trials of three compounds (PM01183, plitidepsin, PM60184) for cancer. It is a global company with subsidiaries in Germany, Italy, France, Switzerland and the United States.
* 1: It is known that there is a tumor-specific chromosomal translocation and a fusion gene derived therefrom in part of a malignant soft tissue tumor. Chromosome translocation is one in which two genes present on different chromosomes are cut and fused with other chromosomes. It is said that fusion genes newly generated by this chromosomal translocation are highly likely to cause tumor generation.
* 2: Calculated by subtracting 1,000 patients with "mesothelioma" from 6,000 patients in "malignant neoplasm of mesothelial and soft tissues" in the Ministry of Health, Labor and Welfare Patient Survey (Heisei 23).
* 3: As of July 2015.
About the outline of approval contents
Product name Yondelis® for intravenous infusion 0.25mg · Yondelis® for intravenous infusion 1 mg
Common name Trabectedin
Efficacy Malignant soft tissue tumor
Dosage / administration Usually, adults receive intravenous drip infusions of 1.2 mg / m 2 (body surface area) once as trabectein over 24 hours and withdraw at least 20 days. Repeat administration with this as one cycle. Incidentally, weight reduction is made according to the condition of the patient.