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NM441是日本新药公司研究开发的新氟喹诺酮抗菌药NM394的前药,口服NM441后由小肠上部吸收时和经肝脏代谢时转变为具抗菌活性的NM394,NM394不仅抗菌谱广、生物利用度高、体内活性强尤其对绿脓杆菌,而且细胞毒性低、向中枢神经系统移行少.日本新药公司于1987年以来先后已在13个国家申请了专利,于1991年11月开始组织了研究会,对本品进行了一系列基础和临床研究.目前日本新药公司和明治公司正在日本联合开发本品,估计已完成Ⅲ期临床研究.现将日本的研究结果介绍如下.
NM441 is a prodrug of the new fluoroquinolone antibacterial NM394 researched and developed by Japan’s new drug company. NM441 is transformed into NM394 with antibacterial activity when it is absorbed by the upper intestine and metabolized by the liver after oral administration of NM441. NM394 not only has wide antibacterial spectrum and high bioavailability, Strong in vivo activity, especially against Pseudomonas aeruginosa, and low cytotoxicity, less migration to the central nervous system .Japanese drug companies in 1987 has been in 13 countries have applied for a patent, in November 1991 began to organize a study, the This product has conducted a series of basic and clinical research.Now Japan’s new drug companies and Meiji company is the joint development of this product in Japan, it is estimated that the Phase III clinical study has been completed now Japan’s findings are as follows.