生物活性

• 描述Streptococcus pneumoniae (pneumococcus) remains the most common cause of community-acquired pneumonia, meningitis, bacteremia, and otitis media. The percentages of these S. pneumoniae isolates that were categorized as susceptible (penicillin-susceptible S. pneumoniae [PSSP]), intermediate, and resistant (penicillin-resistant S. pneumoniae [PRSP]) to penicillin were found to be 93.2%, 5.6%, and 1.2%, respectively. Tedizolid is a new oxazolidinone designed for improved antibacterial potency, especially against linezolid-resistant strains. It is being developed for the treatment of serious infections caused by Gram-positive bacteria, including PRSP. Agar dilution experiments demonstrated that all 28 clinical isolates of PRSP were inhibited by tedizolid at 0.25 μg/ml (MIC (minimal inhibition concentration) range, 0.125 to 0.25 μg/ml). And the MIC₉₀ was 0.25 μg/ml with tedizolid. In mice infected systemically with a lethal inoculum of PRSP, oral administration of tedizolid phosphate was potent for survival at day 7, with 50% effective dose (ED₅₀) values ranging from 3.19 to 11.53 mg/kg of body weight/day. In the PSSP pneumonia model, the ED₅₀ for survival at day 15 was 2.80 mg/kg/day for oral tedizolid phosphate. At a dose of 10 mg/kg once daily tedizolid phosphate, pneumococcal titers in the lungs at 52 h postinfection were approximately 3 orders of magnitude lower with tedizolid phosphate treatment than with no treatment. Lung histopathology showed less inflammatory cell invasion into alveolar spaces in mice treated with tedizolid phosphate than in untreated mice. These results demonstrate that tedizolid phosphate is effective in murine models of PRSP systemic infection and PSSP pneumonia^[2].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01431833	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Trius Investigator Site 001 Orlando, Florida, United States, 32809 United States, Minnesota Trius Investigator Site 002 Minneapolis, Minnesota, United States, 55404 Collapse <<
  NCT02097043	Healthy	Phase 1	Completed	-	Korea, Republic of ... more >> Seoul National University Hospital Seoul, Korea, Republic of Collapse <<
  NCT00761215	Skin Diseases, Infectious ... more >> Skin Diseases, Bacterial Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> Trius Study Site #011 Dothan, Alabama, United States, 36301 United States, California Trius Study site #001 Chula Vista, California, United States, 91911 Trius Study Site #009 Long Beach, California, United States, 92708 Trius Study site #002 Oceanside, California, United States, 92056 Trius Study site #010 Pasadena, California, United States, 91105 Trius Study site 007 San Francisco, California, United States, 94143 Trius Study site 003 San Jose, California, United States, 95124 United States, Georgia Trius Study site 004 Columbus, Georgia, United States, 31904 Trius Study site #006 Ludowici, Georgia, United States, 31316 Trius Study site #005 Savannah, Georgia, United States, 31406 United States, Illinois Trius Study site #012 Springfield, Illinois, United States, 62701 United States, Michigan Trius study sie #008 Detroit, Michigan, United States, 48202 Collapse <<

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• 参考文献

• [1] McCool R, Gould IM, et al. Systematic review and network meta-analysis of tedizolid for the treatment of acute bacterial skin and skin structure infections caused by MRSA. BMC Infect Dis. 2017 Jan 7;17(1):39.

  [2] Activity of tedizolid phosphate (TR-701) in murine models of infection with penicillin-resistant and penicillin-sensitive Streptococcus pneumoniae