Motif BioSciences, Princeton, New Jersey; Rutgers New Jersey Medical School, Trenton, New Jersey.
IHMA, Monthey, Switzerland.
Diagn Microbiol Infect Dis. 2020 May;97(1):115013. doi: 10.1016/j.diagmicrobio.2020.115013. Epub 2020 Feb 5.
Iclaprim is a novel diaminopyrimidine, which inhibits bacterial dihydrofolate reductase, and it is active against Gram-positive pathogens including emerging drug-resistant pathogens. In vitro activity of iclaprim and comparators against 1365 Gram-positive clinical isolates from patients with skin and skin structure infections (SSSI) from the United States, Asia Pacific, Latin America, Europe, Africa or Middle East collected between 2013 and 2017 were tested. Susceptibility testing was performed according to the Clinical and Laboratory Standards Institute (CLSI) guidelines. Minimum inhibitory concentration (MIC) interpretations were based on CLSI criteria. MIC for all S.aureus, methicillin-susceptible S. aureus, methicillin-resistant S. aureus, Streptococcus pyogenes, S. agalactiae, S. anginosus, S. constellatus, S. dysgalactiae and S. intermedius were 0.12, 0.12, 0.5, 0.03, 0.5, ≤0.004, ≤0.004, 0.12, and 0.008 μg/ml, respectively. The MIC for iclaprim was 8 to 32-fold lower than trimethoprim, the only FDA approved dihydrofolate reductase inhibitor, against all Gram-positive isolates including resistant phenotypes. Iclaprim demonstrated lower MICs than trimethoprim against a collection (2013-2017) of Gram-positive clinical isolates from patients with SSSI from the United States, Asia Pacific, Latin America, and Europe.
依拉普利姆是一种新型二氨基嘧啶,可抑制细菌二氢叶酸还原酶,对革兰氏阳性病原体(包括新兴耐药病原体)具有活性。体外活性测试了依拉普利姆和对照药物对 2013 年至 2017 年间从美国、亚太地区、拉丁美洲、欧洲、非洲或中东的皮肤和皮肤结构感染(SSSI)患者中收集的 1365 株革兰氏阳性临床分离株的抑制作用。药敏试验按照临床和实验室标准协会(CLSI)指南进行。基于 CLSI 标准进行最低抑菌浓度(MIC)解释。所有金黄色葡萄球菌、甲氧西林敏感金黄色葡萄球菌、甲氧西林耐药金黄色葡萄球菌、化脓性链球菌、无乳链球菌、咽峡炎链球菌、星座链球菌、缓症链球菌和中间链球菌的 MIC 分别为 0.12、0.12、0.5、0.03、0.5、≤0.004、≤0.004、0.12 和 0.008μg/ml。依拉普利姆的 MIC 比唯一经 FDA 批准的二氢叶酸还原酶抑制剂甲氧西林低 8 至 32 倍,对所有革兰氏阳性分离株(包括耐药表型)均有效。与美国、亚太地区、拉丁美洲和欧洲 SSSI 患者的革兰氏阳性临床分离株(2013-2017 年)的收集相比,依拉普利姆的 MIC 比甲氧西林低。