所属类别： 4毫升/安瓿 1安瓿
包装规格： 4毫升/安瓿 1安瓿
商品药名：MIRIPLA suspension vehicle
本品专用混悬液已于同年8月20日获得批准。2010年1月20日，Miriplatin Hydrate及其专用混悬液同时上市。商標名MIRIPLA suspension vehicle批准日期：2010年1月一般名ヨード化ケシ油脂肪酸エチルエステルIodine addition products of the ethylesters of the fatty acids obtained from poppyseed oil本质上是将碘与罂粟油脂肪酸乙酯结合在一起，定量时含有碘（I：126.90）36.0～41.0%。
它是淡黄色至黄棕色透明粘稠油状液体。 与乙醇(95)，乙醚或氯仿混合。 不溶于水。 它通过空气或光逐渐变成深棕色。粘性27至54mm2/s(20°C)比重d 2020年1.270至1.292处理注意事项根据批次的不同，色调会有一些差异，但如果从浅黄色到黄棕色，则不会出现异常。
该药的延长寿命尚未得到证实。见表2临床结果表表2対象疾患名TE V注)の割合肝細胞癌26.5%(22/83)注)TE V(坏死作用100%或肿瘤减少率100%)作为肝癌治疗的直接作用判定标准
Miriplatin Hydrate is a fat-soluble platinum complex anticancer drug developed by Dainippon Sumitomo Pharmaceutical Co., Ltd., and was approved by the Japanese Ministry of Health, Labor and Welfare on October 16, 2009 for the treatment of hepatocellular carcinoma. The special suspension for this product was approved on August 20 of the same year. On January 20, 2010, Miriplatin Hydrate and its special suspension were launched at the same time.Hepatocellular carcinoma is one of the most common malignant tumors with high recurrence rate in the world. It ranks fifth in the incidence of malignant tumors worldwide, and the third cause of death, and it is increasing year by year, with more than 626,000 people/year.The number of cases in China accounts for about 55% of the total number of cases in the world. In 2005, there were about 66,000 patients with hepatocellular carcinoma in Japan. The onset of hepatocellular carcinoma is characterized by persistent infection of hepatitis C virus or hepatitis B virus leading to chronic hepatitis and cirrhosis, and eventually to hepatocellular carcinoma. Clinically, surgical treatment such as liver resection and transplantation; radiofrequency ablation, percutaneous microwave coagulation therapy, percutaneous ethanol injection therapy, etc; transcatheter arterial chemoembolization (TACE), transcatheter arteries Perfusion therapy; systemic chemotherapy. Among them, TACE was used only when it was unable to perform surgery or local medical treatment, but the proportion in the first treatment was 29.6%, and it was 53.3% in the intrahepatic recurrence treatment. TACE is to inject a mixture of an anticancer drug and an iodinated poppy seed oil into the lesion from the hepatic artery, and at the same time, an embolization substance such as a gelatin sponge is injected to block the artery, and the blood flow of the artery is cut off, thereby achieving the purpose of causing tumor necrosis. Anticancer drugs for TACE include doxorubicin hydrochloride, epirubicin hydrochloride, mitomycin, cisplatin, and net statin. Among them, the platinum anticancer drug cisplatin is widely used for its high anticancer activity and broad-spectrum anticancer effect, and it also shows good clinical effect on hepatocellular carcinoma, but its water-soluble characteristics make it use iodine poppy. The physical stability of the carrier oil is seriously affected; the net statin ester is the only one used as the carrier of the ethyl ester of iodinated poppy-seed oil fatty acid The anticancer drug approved by the drug has been approved since its listing in 1994, but the drug may cause problems such as hepatic artery vascular injury and irreversible effects on the hepatobiliary system, which may affect future treatment and prognosis. There are hidden dangers in security. Therefore, it is a new target for drug research and development to find a drug with high affinity for iodinated poppy oil fatty acid ethyl ester, anticancer effect no less than net statin ester, safe prognosis and hidden danger.Miriplatin Hydrate is a fat-soluble platinum complex developed by Maeda et al., National Institute of Cancer Research, Japan. It has high affinity with iodinated poppy oil fatty acid ethyl ester and can be stably dissolved in iodinated poppy oil fatty acid ethyl ester to form a sustained release. The drug is selectively and long-term retained in the cancer site after administration through the hepatic artery, and the drug is slowly released, and the anticancer effect is excellent. Based on the research of Tian et al.Sumitomo has been discussing the synthesis, physical properties, formulation and non-clinical trials of this product since the 1990s, and based on the results obtained from non-clinical trials, since 1994 Japan conducts clinical trials on patients with hepatocellular carcinoma. Phase I clinical trials began in October 1994, Phase II Phase A clinical trials began in July 1998, and Phase II Phase B clinical trials began in April 2002. Clinical trials have shown that this product shows good anti-tumor effects not only for patients who are treated for the first time, but also for patients with hepatocellular carcinoma who have relapsed after treatment with other methods such as hepatectomy.Moreover, the adverse reactions of this product are all known general adverse reactions of this therapy, and these adverse reactions can be tolerated as long as the patients receive the treatment of the drug in a medical institution that is proficient in the therapy. Based on the results of these three clinical trials and the follow-up test results of Phase II B-phase clinical trials, this product was finally approved by the Ministry of Health, Labor and Welfare of Japan.Pharmacodynamics and pharmacologyThe rat liver cancer model was transplanted with liver transplanted mouse hepatoma cell line AH109A or human hepatoma cell line Li-7 to eva luate the inhibitory effect of the suspension on proliferation of cancer cells in vivo.The results showed that the suspension of this product inhibited the proliferation of cancer cells in a dose-dependent manner, and the tumor cell proliferation rate was significantly decreased when the product was 20 mg/mL in the suspension.The single-dose administration of this product suspension also has a dose-dependent anti-tumor effect on the same liver cancer model.This product is an anticancer drug dissolved in special iodinated poppy oil fatty acid ethyl ester and intrahepatic artery. It has high affinity with iodinated poppy oil fatty acid ethyl ester and is retained in hepatic artery after administration. At the tumor site, the platinum component in the suspension can be slowly released into the blood or tissue for a long time, and the platinum divalent compound binds to the DNA, inhibits the proliferation of the cancer cell by preventing DNA synthesis, and improves the anticancer effect.Clinical trial resultsThe results of phase I clinical trials show that the maximum tolerated dose of this product is 20mg/mL or more (the maximum dose is 6mL); the total platinum concentration in the blood after administration is extremely low, which can be maintained for a long time; the degree of adverse reactions is light and controllable And in the tolerance range. The 1-year survival rate of this product is 63.6%, and the 2-year survival rate is 38.2%.The results of Phase II Phase A clinical trials showed that the total platinum concentration (ng) in the blood after administration of this product was extremely low, which was trace amount and long-lasting. The Cmax decreased to about 17% in about 1 year after administration. No serious adverse reactions of grade 4 were observed, and almost all of the adverse reactions seen disappeared 4 to 6 weeks after administration, which was controllable and within the tolerance range. The curative effect (TE) of this product on hepatocellular carcinoma is good, and the CR rate is 60%.The results of Phase II B clinical trials show that this product is equivalent to net statin and safer. The total platinum concentration in the blood (average value) was 9.6 and 12.9 ng/mL after the first and the second administration, respectively, and the platinum concentration (average value) separated by methanol was 1.17 and 1.19 ng/mL, respectively. The survival rates of this product in 1st, 2nd, and 3rd years were 90.1%, 75.9%, and 58.4%, respectively. The survival rates of the control group were 97.4%, 70.3%, and 48.7%, respectively.Clinical trials have shown that this product has a good anticancer effect, whether it is the first time to receive this treatment for hepatocellular carcinoma, or some relapsed patients who have undergone other treatments such as liver resection. Moreover, side effects are common side effects in such treatments, and they are treated in a medical institution proficient in such treatments, and these side effects are controlled within the tolerance range.