艾拉普林的研究进展
Research Progress of Iclaprim
孙燕 1陈萍 1邢俊香1
作者信息
- 1. 淄博市中心医院,山东 淄博 255000
- 折叠
摘要
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.
Abstract
Antibiotic resistance is an ever-increasing global threat to public health by jeopardizing the treatment of infectious dis-eases.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 infec-tions and hospital-acquired pneumonia in Gram-positive bacteria and phase III trials have been completed.Studies have shown that Icl-aprim 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 treat-ment of new therapeutic drugs for Gram-positive bacteria resistant bacterial infections.
关键词
艾拉普林/革兰氏阳性耐药菌/皮肤感染/软组织感染/医院获得性肺炎Key words
Iclaprim/Gram-positive bacteria/Skin infections/Skin structure infections/Nosocomial pneumonia引用本文复制引用
出版年
2024
NETL
NSTL
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