Recently (November 7th), the official website of the China National Center for Drug Evaluation (CDE) showed that Chengdu Yuandong Biopharmaceutical Co., Ltd.'s application for the marketing of injection grade naprolimus mesylate, classified as Class 3, has been accepted. According to public information, the indications of this product are for the treatment of acute pancreatitis, chronic pancreatitis with acute exacerbation, postoperative acute pancreatitis, acute pancreatitis after pancreatography, and acute traumatic pancreatitis; Used for the treatment of disseminated intravascular coagulation (DIC); 3. Used to prevent blood clotting during extracorporeal circulation.

Naprolimus mesylate is a strong and broad-spectrum serine protease inhibitor. This product was first launched in Japan for the prevention and treatment of disseminated intravascular coagulation (DIC), improvement of acute symptoms of pancreatitis, and anticoagulation during extracorporeal circulation. In March 2020, according to overseas media reports, Professor Junichiro Inoue of the Medical Research Institute of the University of Tokyo and others issued a statement saying that the drug "Naprolimus", which is mainly used to treat acute pancreatitis, has the effect of preventing novel coronavirus from entering human cells. At present, Japan has included Naprolimus as a candidate treatment drug for COVID-19. Jiangsu Durui Pharmaceutical Co., Ltd. has developed the first domestically replicated injection of naprolimus mesylate, which will fill the gap in the field of DIC prevention and treatment in China. To provide a safe and effective new drug for the prevention of severe pancreatitis, postoperative pancreatitis, and hemodialysis for high-risk bleeding prone patients.

Naprolimus mesylate is a serine protease inhibitor. Initially, it was not marketed as an anticoagulant, but rather as a treatment for pancreatitis. It has a strong inhibitory effect on pancreatic derived proteolytic enzymes such as trypsin, phospholipase A2, and elastase. At the same time, NM also has a multi-target anticoagulant effect, acting on key coagulation factors such as thrombin, VIIa, Xa, and XIIa, and can be used for anticoagulation during extracorporeal circulation. NM begins to degrade after injection into the blood during extracorporeal circulation, and blood purification also removes a corresponding proportion of NM through diffusion, convection, and adsorption. A small amount of NM enters the body and is rapidly degraded by the liver, with a half-life of only 5-8 minutes, which has little impact on the coagulation function in the body. Therefore, NM has local anticoagulation characteristics in vitro. Compared with other anticoagulants used for systemic anticoagulation, NM significantly reduces the incidence of bleeding. It is not only suitable for routine blood purification anticoagulation, but also for patients with bleeding risk and active bleeding. This provides a new solution for blood purification therapy for bleeding patients. Plan.

The characteristic of naprolimus is that its half-life is only 8 minutes, which is only 1/8-1/15 of conventional anticoagulants; There are multiple metabolic pathways, which can be metabolized in the liver and blood. It can still be safely used when patients experience organ failure; It can act on multiple sites such as the coagulation fibrinolysis system, kallikrein system, complement system, etc., with outstanding anticoagulant advantages; The incidence of bleeding complications is low, only 1/6 of that of heparin.

Nalolimus can strongly inhibit activated coagulation factors such as factor IIa, factor Xa, and factor XIa, exerting non anticoagulant effects mediated by antithrombin III.

The original research was developed by Torii Pharmaceutical Co., Ltd. in Japan and was launched in 1986. It is mainly used in clinical practice to treat pancreatitis and disseminated intravascular coagulation (DIC). According to the situation of domestic generic drugs, it is understood that Jiangsu Durui Pharmaceutical Co., Ltd. has injected nalolimus mesylate (NM) (trade name: Fudu) for injection ®） On September 30, 2020, it was approved for market by the NMPA in China, which is the first domestically replicated and an ideal anticoagulant for extracorporeal circulation. The drug's original research has not yet been launched in China.
This product has a strong selective inhibitory effect on trypsin like serine proteases such as trypsin, blood fibrin, fibrin, kallikrein (angiotensin releasing enzyme), and classical pathways of complement system C1r, C1S, etc. It also has an inhibitory effect on trypsin binding to a2 macroglobulin in vitro, and can inhibit the increase in pancreatic enzyme activity caused by pancreatitis and the enzyme activity entering the blood. It can reduce the mortality rate of experimental pancreatitis caused by retrograde injection of trypsin, enterokinase, and endotoxin through the pancreatic duct. The relevant guidelines recommend sufficient application in the early stage of acute pancreatitis, with good market prospects.

Natrolimus Mesylate Injection (NM) was originally developed by Torii Pharmaceutical Co., Ltd. in Japan and is included in the "Japanese Medical Products" and "Japanese Pharmacopoeia". It is recommended in the "Japanese Blood Purification Therapy Manual" and "Japanese Guidelines for Diffuse Intravascular Coagulation Therapy". Nalolimus mesylate for injection is a clinically recognized drug, which will bring a safe and effective new drug to patients in the field of blood purification in China. It has broad prospects and is expected to become a heavyweight potential product in the in vitro anticoagulation market.

Source: https://pharm.jgvogel.cn/c1461814.shtml