[图]盐酸苯达莫司汀注射液Treakisym(bendamustine hydrochloride)

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卫材已在日本推出抗癌注射制剂Treakisym（100毫克，通用名为盐酸苯达莫司汀），该药用于治疗低度B细胞性非霍奇金淋巴瘤。

Treakisym是卫材在日本市场推出的第一种抗癌药，在此之前这种药物已经在美国市场上销售。卫材表示，Treakisym是一种新型抗癌制剂，它不但可以发挥氮芥源烷基化物的作用，还可以起到类似于反新陈代谢规律的作用。

在日本当地进行的临床实验结果显示，Treakisym疗效明显，应答率高，患者用药后病情无恶化生存期也得到延长。

目前，卫材合作方——SymBio 制药公司正在日本开展Treakisym 的一项II期临床实验，受试者为复发/难治型中-高度B细胞性非霍奇金淋巴瘤患者以及未接受过治疗的多发性骨髓瘤患者，这是扩大药物适应症实验项目的组成部分之一。

随着首款抗癌药的推出，卫材计划进一步扩充其抗癌药产品线，乳腺癌治疗药Eribulin则是其中之一

盐酸苯达莫司汀（Bendamustine Hydrochloride）化学名为4-[5-[双（2-氯乙基）氨基]-1-甲基苯并咪唑-2-基]丁酸盐酸盐。早在上世纪60年代，盐酸苯达莫司汀即由前东德研制而成，并被广泛应用，但直到冷战结束，该药才在欧洲进行了多项单药或联合其他药物治疗多种血液系统恶性肿瘤或实体瘤的临床研究，疗效非常可观。
到目前为止，盐酸苯达莫司汀单药或联合治疗方案已被欧美临床指南指定为多种血液系统恶性肿瘤的一线或二线治疗选择。2003年，盐酸苯达莫司汀在德国上市，商品名为“Ribomustin”。在美国上市的盐酸苯达莫司汀商品名为“Treanda”，由Cephalon公司提出上市申请，并于去年通过优先审批程序获得FDA批准。
【适应症】

2008年3月，FDA首先批准盐酸苯达莫司汀用于治疗慢性淋巴细胞性白血病（CLL）。同年10月，FDA又批准了该药的第2个适应证，即在利妥昔单抗（rituximab，美罗华）或含利妥昔单抗方案治疗过程中，或者治疗6个月内，病情仍然进展的惰性B细胞非霍奇金淋巴瘤（NHL）患者。
【药理及药代动力学】

盐酸苯达莫司汀的确切作用机制尚不十分清楚，但已知该药是携带一个嘌呤样苯并咪唑环的氮芥衍生物，兼具烷化剂和嘌呤类似物（抗代谢药）的双重作用机制。盐酸苯达莫司汀能通过几种不同途径导致细胞死亡，而且对静止期和分裂期细胞均有效。
盐酸苯达莫司汀血浆蛋白结合率为94%～96%，数据显示该药一般不会与其他高蛋白结合药物相互置换。盐酸苯达莫司汀平均稳态分布容积约为25L，其全血/血浆浓度比为0.84～0.86。盐酸苯达莫司汀主要通过水解反应进行代谢，同时形成细胞毒性较低的代谢产物。该药经CYP1A2代谢途径可产生M3和M4两种活性代谢产物，但两者血浆浓度只分别相当于母体化合物的1/10和1/100，因此，可以推测苯达莫司汀的细胞毒性作用主要来自于其本身，而非其代谢物。
【禁忌症】 对盐酸苯达莫司汀及甘露醇过敏者禁用。
【药物相互作用】

与CYP1A2抑制剂（如氟伏沙明，环丙沙星等）合用时，有可能会升高苯达莫司汀血浓度，并使其代谢物M3和M4浓度降低；与CYP1A2诱导剂（如奥美拉唑，抽烟等）合用时，有可能会降低苯达莫司汀血浓度，并使其代谢物M3和M4浓度升高。
【不良反应】

苯达莫司汀常见不良反应包括恶心、呕吐、腹泻、疲乏、虚弱、皮疹、搔痒、一些感染症状和体征（如持续咽喉疼痛、发热和寒战）、容易碰伤/出血以及口腔溃疡等；严重不良反应可能还有骨髓抑制、肿瘤溶解综合征等。苯达莫司汀可能引起轻微或严重过敏反应，患者在给药过程中或给药后初期可能出现皮疹、面部肿胀、呼吸困难等过敏症状。苯达莫司汀可能对胎儿造成影响，因此，女性治疗过程中及治疗后3个月内，应采取适当避孕措施及停止哺乳。
【剂量及用药】 苯达莫司汀冻干粉针呈白色至灰白色，规格为100mg/支。该药储存温度不应超过30℃，避光保存，使用前临时配制。
配制流程：该药每100mg须先溶于20ml无菌注射用水，充分振摇直到完全溶解成澄清、无色或淡黄色溶液，溶解时间一般不超过5分钟，溶解后浓度为5mg/ml。在溶解后30分钟之内，根据需要抽取适量苯达莫司汀水溶液，转移至500ml氯化钠注射液（0.9%）或葡萄糖氯化钠注射液（2.5%/0.45%）中，并确保苯达莫司汀在注射液中的最终浓度在0.2～0.6mg/ml之间。配制好的注射液可在2～8℃冷藏保存24小时，或在室温及自然光下保存3小时。

苯达莫司汀治疗CLL时，以28天为一个治疗周期，一般需要6个治疗周期。在每个治疗周期的第一天和第二天给药，推荐剂量为100mg/m2。该药经静脉滴注给药，每次给药时间不应少于30分钟。
苯达莫司汀治疗NHL时，以21天为一个治疗周期，一般需要8个治疗周期。在每个治疗周期的第一天和第二天给药，推荐剂量为120mg/m2。每次给药时间不应少于60分钟。
【患者咨询】
用药前应告知主诊医生有关过敏史、详细的用药史及其他伴发疾病，特别是血液/骨髓病、肾脏病、肝病、感染疾病等，同时应与医生详细讨论服药的风险及受益情况，避免与其他可能产生不良相互作用的药物合用。该药可能使现有感染加重，因此，在未征得医生同意前，患者不要自行进行疫苗接种；同时应避免与近期口服过脊髓灰质炎疫苗或通过鼻吸入给予流感疫苗的人群，又或者是其他传染病（如水痘、流感）患者接触。

Eisai Co., Ltd. (Headquarters: Tokyo, President & CEO: Haruo Naito, “Eisai”) today launched the anticancer agent TREAKISYM® Injection 100 mg (generic name: bendamustine hydrochloride) in Japan as a treatment for low-grade B-cell non-Hodgkin\'s lymphoma and mantle cell lymphoma. TREAKISYM® is the first anticancer agent for Eisai to launch in Japan, and although it is already available in the United States, its Japan launch marks the company\'s fully-fledged entry into the Japanese oncology market.

SymBio Pharmaceuticals Limited (Headquarters: Tokyo, President & CEO: Fuminori Yoshida, “SymBio”) received marketing approval for TREAKISYM® on October 27 of this year. The drug was today added to Japan’s National Health Insurance drug price list and will be marketed by Eisai in Japan based on a licensing agreement concluded between the two companies.

Eisai has established a Japan-based oncology promotion framework under which oncology information specialists have been assigned to each area and all of the approximately 1400 medical representatives (MRs) stationed around the country will provide information on anticancer therapies. The company will also work to ensure that a use results survey (all-case surveillance), a condition under which TREAKISYM® was approved, is carried out smoothly and promote the safe and efficacious use of the drug.

TREAKISYM® is a novel anticancer agent that exhibits nitrogen mustard-derived alkylating activity and antimetabolic-like activity. Clinical studies conducted in Japan showed that the agent offers excellent efficacy, has a high response rate, and significantly extends the duration of progression-free survival. More importantly, it is the first single agent for which patients with mantle cell lymphoma demonstrated a complete response. While the most frequently reported adverse reactions associated with TREAKISYM® include myelosuppression, nausea, vomiting, infection, vasculitis and angialgia, the agent maintains a manageable and highly tolerable safety profile. In Japan, SymBio is currently conducting Phase II clinical studies with the agent in relapsed and refractory intermediate- and high-grade B-cell non-Hodgkin’s lymphoma and untreated multiple myeloma as part of an indication expansion program.

Non-Hodgkin\'s lymphoma strikes an estimated 12,000 people in Japan each year, with the number of cases increasing in recent years. It is well known that many low-grade non-Hodgkin’s lymphoma patients are prone to repeated relapse after responding to initial treatment, making further treatment difficult despite extended overall survival. Mantle cell lymphoma is one of the rarest types of lymphoma. As most patients present with advanced stage disease, a common standard of care has yet to be established.

Eisai positions oncology as a therapeutic area of focus. Following the debut of its first anticancer agent TREAKISYM®, Eisai plans to continue to expand its portfolio of oncology products with agents such as eribulin (generic name), the company\'s first in-house developed anticancer agent currently under regulatory review for the treatment of breast cancer, thereby making contributions to addressing the diversified needs of cancer patients and their families.

1. About Bendamustine Hydrochloride
Bendamustine hydrochloride is an anticancer agent originally synthesized by German (formerly ‘East German’) pharmaceutical company Jenapharm and is marketed in Europe under the brand names Ribomustin® and Levact® as a treatment for non-Hodgkin\'s lymphoma, multiple myeloma and chronic lymphocytic leukemia. In the United States, the agent is marketed under the brand name TREANDA® as a treatment for chronic lymphocytic leukemia and relapsed indolent B-cell non-Hodgkin\'s lymphoma.
Eisai concluded an exclusive licensing agreement with SymBio in August 2008 concerning the joint development and marketing of bendamustine hydrochloride in Japan, which was followed by a subsequent agreement between the two companies in May 2009 concerning the development and marketing of the agent in Singapore and South Korea. The agent has been marketed in Singapore by Eisai’s Singapore subsidiary Eisai (Singapore) Pte. Ltd. since September of 2010 under the brand name of Symbenda® for the treatment of low-grade non-Hodgkin’s lymphoma and chronic lymphocytic leukemia.

2. TREAKISYM® Product Outline

Product Name:
TREAKISYM® Injection 100 mg
Generic Name:

Bendamustine Hydrochloride
Indications and Usage:

For the treatment of relapsed or refractory:
• Low-grade B-cell non-Hodgkin\'s lymphoma
• Mantle cell lymphoma
Dosage and Administration:

The usual adult dose of bendamustine hydrochloride is 120 mg/m2 (body surface area) infused intravenously on Days 1 and 2 of repeated 21 day cycles. The dose may be reduced appropriately according to the condition of the patient.
National Health Insurance Drug Price Standard:

TREAKISYM® Injection 100 mg
3. Product Image