Lofland Denene, Difuntorum Stacey, Waller Andrew, Clements John M, Weaver Mellany K, Karlowsky James A, Johnson Kirk
Genesoft Pharmaceuticals, Inc., 7300 Shoreline Court, South San Francisco, CA, USA.
J Antimicrob Chemother. 2004 Apr;53(4):664-8. doi: 10.1093/jac/dkh129. Epub 2004 Feb 18.
BB-83698 is a peptide deformylase inhibitor currently in clinical trials in Europe. The purpose of this study was to provide additional susceptibility data from clinical isolates, including drug-resistant strains.
The in vitro activities of BB-83698 and comparators were determined against 281 streptococci, 154 Staphylococcus aureus, 110 Haemophilus influenzae and 50 Moraxella catarrhalis strains selected for their resistance phenotypes. Broth microdilution MICs and MBCs were determined according to NCCLS guidelines.
The MIC90s were 0.25-0.5 mg/L for S. pneumoniae, including penicillin-, erythromycin-, levofloxacin- and multidrug-resistant strains. The MIC90s for Streptococcus pyogenes and Streptococcus agalactiae were 0.12 mg/L and for viridans streptococci, the MIC90 was 0.5 mg/L. Against S. aureus, including oxacillin- and levofloxacin-resistant strains, and vancomycin-intermediate strains, the MIC90 was 8 mg/L. Against beta-lactamase-negative and -positive H. influenzae, the MIC90s were 32 and 64 mg/L, respectively, and against both beta-lactamase-negative and -positive M. catarrhalis the MIC90 was 0.12 mg/L. In MBC studies, the ratio of MBC/MIC was 1:1 or 2:1 against 31% of S. pneumoniae, 33% of S. aureus, 63% of H. influenzae and 9% of M. catarrhalis.
Although BB-83698 has reduced in vitro activity against H. influenzae, it is a potent antimicrobial with excellent activity against streptococci and Moraxella.
BB - 83698是一种肽脱甲酰基酶抑制剂,目前正在欧洲进行临床试验。本研究的目的是提供来自临床分离株(包括耐药菌株)的更多药敏数据。
测定BB - 83698及对照药物对281株链球菌、154株金黄色葡萄球菌、110株流感嗜血杆菌和50株卡他莫拉菌的体外活性,这些菌株根据其耐药表型进行选择。根据美国国家临床实验室标准委员会(NCCLS)指南测定肉汤微量稀释法的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)。
对于肺炎链球菌,包括对青霉素、红霉素、左氧氟沙星耐药及多重耐药菌株,MIC90为0.25 - 0.5mg/L。化脓性链球菌和无乳链球菌的MIC90为0.12mg/L,草绿色链球菌的MIC90为0.5mg/L。对于金黄色葡萄球菌,包括对苯唑西林和左氧氟沙星耐药菌株以及万古霉素中介菌株,MIC90为8mg/L。对于β - 内酰胺酶阴性和阳性的流感嗜血杆菌,MIC90分别为32mg/L和64mg/L,对于β - 内酰胺酶阴性和阳性的卡他莫拉菌,MIC90均为0.12mg/L。在MBC研究中,MBC/MIC比值为1:1或2:1的情况分别见于31%的肺炎链球菌、33%的金黄色葡萄球菌、63%的流感嗜血杆菌和9%的卡他莫拉菌。
尽管BB - 83698对流感嗜血杆菌的体外活性有所降低,但它是一种对链球菌和卡他莫拉菌具有优异活性的强效抗菌药物。