艾拉普林的研究进展

Research Progress of Iclaprim

抗菌药物耐药性已成为全球面临的主要健康威胁,临床迫切需要新的抗菌药物以应对革兰氏阳性耐药菌感染。艾拉普林(英文名iclaprim)是Arpida公司开发的抗革兰氏阳性菌新药,是一种二氢叶酸还原酶抑制剂,现已获批用于治疗革兰氏阳性菌的皮肤、软组织感染和院内获得性肺炎的临床试验,目前已完成III期临床试验。研究表明,艾拉普林具有良好的组织分布,在体内、体外均有良好的抗菌活性,抗革兰氏阳性菌活性非劣效万古霉素,不良反应发生率与万古霉素类似,无肾毒性,抗菌谱包括全部革兰氏阳性菌、部分革兰氏阴性菌、非典型病原体、卡氏肺孢子。艾拉普林因体内分布广、蛋白结合率高、肺内浓度、药物不良反应少、良好耐受性等特点,有望成为治疗革兰氏阳性耐药菌感染的治疗药物。本研究综述了艾拉普林药理学、抗病原微生物活性、抗菌活性、药代动力学等各方面的研究进展,旨在为开发和治疗革兰氏阳性耐药菌感染的新兴治疗药物提供借鉴。

Antibiotic resistance is an ever-increasing global threat to public health by jeopardizing the treatment of infectious diseases.An emergency demand for new mechanism antimicrobial agents have been launching to effectively treat the infections caused by resistant strains.Iclaprim a new Gram-positive bacteria drug developed by Arpida,a novel 2,4-diaminopyrimidine with potent rapidly bactericidal activity against Gram-positive pathogens.Its clinical trials have been approved for the treatment of skin and soft tissue infections and hospital-acquired pneumonia in Gram-positive bacteria and phase III trials have been completed.Studies have shown that Iclaprim has good tissue distribution,good antibacterial activity in vivo and in vitro,and Gram-positive bacteria activity is non-inferior to vancomycin.The incidence of adverse reactions is similar to that of vancomycin,no nephrotoxicity.The antimicrobial spectrum includes all Gram-positive bacteria,some Gram-negative,atypical pathogens and pneumocystis carinii.Because of its wide distribution in the body,high protein binding rate,high pulmonary concentration,less adverse drug reactions and good tolerance,Iclaprim is expected to become a therapeutic drug for the treatment of Gram-positive bacteria resistant bacterial infections.In this study,the pharmacological,antimicrobial,antimicrobial,and pharmacokinetics aspects of etopol were reviewed,to provide reference for the development and treatment of new therapeutic drugs for Gram-positive bacteria resistant bacterial infections.